Compounds active at the serotonergic 5-HT 2a receptor

Abstract

The present disclosure relates to compounds of formula (I), their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.

Description

[0001] COMPOUNDS ACTIVE AT THE SEROTONERGIC 5-HT2ARECEPTOR

[0002] Cross-reference

[0003] This application claims priority to Australian provisional application no. 2023903954 (filed on 6 December 2023), the entire contents of which is incorporated herein by reference.

[0004] Field of the invention

[0005] The present disclosure relates generally to compounds active at the serotonergic 5-HT2A receptor that may be useful in the treatment of mental illness or central nervous system disorders. The disclosure also relates to methods of synthesis of the compounds, compositions comprising the compounds and to methods for their use

[0006] Background of the invention

[0007] Mental illness covers many neuropsychiatric disorders which cause enormous burden on the lives of their sufferers. Diagnoses such as treatment resistant depression, major depressive disorder, eating disorders, substance abuse disorders, post-traumatic stress disorder, obsessive compulsive disorder, attention deficit disorders, schizophrenia, and others can cause such devastating symptoms that many sufferers lose the capability of leading a normal life.

[0008] A variety of serotonergic drugs such as antidepressants, serotonin reuptake inhibitors, monoamine oxidase inhibitors, selective serotonin reuptake inhibitors, and others are commercially available to treat mental illnesses. Unfortunately, in many indications, these therapeutics provide limited benefit when compared to a placebo. Additionally, these therapeutics can result in a wide range of side effects including loss of libido, insomnia, fatigue, weight gain, and others. In spite of their limited efficacy, these drugs continue to be used to treat neuropsychiatric conditions as well as a broad range of auxiliary medical indications. There have been limited advances in new treatment options since many of these drugs were released, and the pharmaceutical industry has come under increased financial pressure to de-emphasise neuroscience programmes entirely. The unmet need for more efficacious mental health treatment is on the rise, and the global COVID-19 pandemic is likely to increase disease burden around the world. In the 1950s and 1960s, the use of psychedelic drugs to treat various mental illnesses was extensively explored, and these substances showed promise as treatments for many diseases of the central nervous system (CNS). Following decades of prohibition, scientific research into the application of psychedelics as treatments for mental illnesses has been gaining momentum. The serotonergic psychedelic agent psilocybin has been designated a Breakthrough Therapy by the FDA for the treatment of major depressive disorder (2019) and treatment-resistant depression (2018). Psilocybin is the prodrug compound produced by more than many species of mushrooms known collectively as psilocybin mushrooms or “magic mushrooms”. Psilocybin is rapidly metabolized to the bioactive compound psilocin, which produces a state of altered consciousness including changes in perception, visual hallucinations, and distorted sense of space, time, and self. Many patients report spiritual or “mystical” experiences which have profound and lasting impact on the patients’ mood and behaviour. Psilocybin has shown promise in more than 50 clinical trials for neuropsychiatric indications, including numerous anxiety disorders, obsessive- compulsive disorder, anorexia nervosa, alcohol dependence, and tobacco addiction. Psilocybin and other psychedelic compounds such as N,N-dimethyltryptamine (DMT) and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) have both immediate and persistent effects on mental state, with the latter extending far beyond the duration of action, possibly as a result of their ability to incite increased neuroplasticity, promote neural outgrowth, and increase spine density of the synaptic neurons in the brain. To date, psilocybin remains classified as a controlled substance and / or drug of abuse in most countries under national drug laws. However, clinical investigations have recently led to increased awareness of the potential for psychedelic drugs as breakthrough therapies to treat CNS diseases of enormous unmet medical need. Despite its therapeutic potential, psilocybin and other psychedelics remain scheduled drugs of abuse in most countries and the commercial path to market for these drugs as medicines is uncertain. As an adjunct to psychotherapy, the long duration of action of psilocybin and LSD make treatment sessions costly and impractical for broad implementation. In spite of a long history of safe human use, several adverse events have been reported in clinical trials, and it is possible that these may be attributed to signalling bias at 5-HT2A (the primary target) or off-target activity at, for example, 5-HT2B receptors (a cardiac liability antitarget) or 5-HT1A (an anxiolytic target) or 5-HT2C receptors (a disease-relevant target for obesity and some genetic epilepsies, for example). Naturally-occurring psychedelics provide important lead structures for a new generation of neurotherapeutic agents with novel mechanisms of action and / or superior clinical efficacy to currently available neuropsychiatric medications. In view of the foregoing there is an ongoing need to develop new compounds which may be useful in the treatment of mental illness or central nervous system disorders. Reference to any prior art in the specification is not an acknowledgment or suggestion that this prior art forms part of the common general knowledge in any jurisdiction or that this prior art could reasonably be expected to be understood, regarded as relevant, and / or combined with other pieces of prior art by a skilled person in the art. Summary of the invention In one aspect the present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein L is selected from C1-4 alkylene, C2-4 alkenylene and C2-4 alkynylene; R1is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10 heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4- C14 alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R2is independently selected from hydrogen, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6haloalkyl, C3-8cycloalkyl, C4-14alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6 heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; alternatively R1and R2together with the atoms to which they are attached form a C3-8heterocycloalkyl including 0, 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR11, said C3-8heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-8alkylamino, C1-8alkylsulfonyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R3is selected from hydrogen, C1-6alkyl, C3-8cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R3and one of R1and R2together with the atoms to which they are attached form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; each R11is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl, and C3-7heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl and C3-7heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R12, C(O)N(R12)2, OR12, N(R12)2, NO2, SR12and SO2R12, said C3-C7cycloalkyl and C3-7heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12; each R12is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, CN, OR13, N(R13)2, SR13, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, C4-16alkyleneheteroaryl; said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12 aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13and SO2R13, said C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4- 16 alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein at least one of R4, R5, R6and R8is other than hydrogen. In another aspect the present disclosure provides a medicament comprising a compound according to any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. In another aspect the present disclosure provides a pharmaceutical composition comprising a compound according to any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, and a pharmaceutically acceptable excipient. In another aspect the present disclosure provides a pharmaceutical composition comprising a compound according to any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, an additional therapeutic agent, and a pharmaceutically acceptable excipient. In another aspect the present disclosure provides a method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) as defined in any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. In another aspect the present disclosure provides a method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) as defined in any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, in combination with another known agent useful for treatment of a disease, disorder or condition by activation of a serotonin receptor. In another aspect the present disclosure provides a method of treating a mental illness, the method comprising administering to a subject in need thereof a compound of formula (I) as defined in any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. In some embodiments, the mental illness is selected from anxiety disorders; depression; mood disorders; psychotic disorders; impulse control and addiction disorders; drug addiction; obsessive-compulsive disorder (OCD); post-traumatic stress disorder (PTSD); stress response syndromes; dissociative disorders; depersonalization disorder; factitious disorders; sexual and gender disorders; somatic symptom disorders; hallucinations; delusions; psychosis; and combinations thereof. In another aspect the present disclosure provides a method for treating a central nervous system (CNS) disease, disorder or condition and / or a neurological disease, disorder or condition, the method comprising administering to a subject in need thereof a compound of formula (I) as defined in any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof. In some embodiments, the CNS disease, disorder or condition and / or neurological disease, disorder or condition is selected from neurological diseases including neurodevelopmental diseases and neurodegenerative diseases such as Alzheimer’s disease; presenile dementia; senile dementia; vascular dementia; Lewy body dementia; cognitive impairment, Parkinson’s disease and Parkinsonian related disorders such as Parkinson dementia, corticobasal degeneration, and supranuclear palsy; epilepsy; CNS trauma; CNS infections; CNS inflammation; stroke; multiple sclerosis; Huntington’s disease; mitochondrial disorders; Fragile X syndrome; Angelman syndrome; hereditary ataxias; neuro-otological and eye movement disorders; neurodegenerative diseases of the retina amyotrophic lateral sclerosis; tardive dyskinesias; hyperkinetic disorders; attention deficit hyperactivity disorder and attention deficit disorders; restless leg syndrome; Tourette's syndrome; schizophrenia; autism spectrum disorders; tuberous sclerosis; Rett syndrome; cerebral palsy; disorders of the reward system including eating disorders such as anorexia nervosa and bulimia nervosa; binge eating disorder, trichotillomania, dermotillomania, nail biting; migraine; fibromyalgia; and peripheral neuropathy of any etiology, and combinations thereof. In another aspect the present disclosure provides a method for increasing neuronal plasticity and / or increasing dendritic spine density, the method comprising contacting a neuronal cell with a compound of formula (I) as defined in any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, in an amount sufficient to increase neuronal plasticity and / or increase dendritic spine density of the neuronal cell. In another aspect the present disclosure provides methods of treating weight, comprising administering an effective amount of a compound of the invention to a subject in need thereof. Treatment of weight may include treating weight gain; weight loss; metabolic disorder; weight gain associated with pharmaceutical intervention; weight gain associated with a mental illness (including those described herein); eating disorders such as anorexia, bulimia, cachexia, etc.; eating behaviour; obesity; diabetes; insulin resistance; pre-diabetes; glucose intolerance; hyperlipidemia; and cardiovascular disease. In another aspect the present disclosure provides a method for activating a serotonin receptor in a cell, either in a biological sample or in a patient, comprising administering a compound of formula (I) as defined in any one of the herein disclosed embodiments to the cell. Any embodiment herein shall be taken to apply mutatis mutandis to any other embodiment unless specifically stated otherwise. The present disclosure is not to be limited in scope by the specific embodiments described herein, which are intended for the purpose of exemplification only. Functionally-equivalent products, compositions and methods are clearly within the scope of the invention, as described herein. Further aspects of the present invention and further embodiments of the aspects described in the preceding paragraphs will become apparent from the following description, given by way of example. Detailed description of the embodiments It will be understood that the invention disclosed and defined in this specification extends to all alternative combinations of two or more of the individual features mentioned or evident from the text or drawings. All of these different combinations constitute various alternative aspects of the invention. Definitions For purposes of interpreting this specification, terms used in the singular will also include the plural and vice versa. As used herein, except where the context requires otherwise, the term "comprise" and variations of the term, such as "comprising", "comprises" and "comprised", are not intended to exclude further additives, components, integers or steps. The terms "treatment" or "treating" of a subject includes delaying, slowing, stabilizing, curing, healing, alleviating, relieving, altering, remedying, less worsening, ameliorating, improving, or affecting the disease or condition, the sign or symptom of the disease or condition, or the risk of (or susceptibility to) the disease or condition. The term "treating" refers to any indication of success in the treatment or amelioration of an injury, pathology or condition, including any objective or subjective parameter such as abatement; remission; lessening of the rate of worsening; lessening severity of the disease; stabilization, diminishing of signs or symptoms or making the injury, pathology or condition more tolerable to the individual; slowing in the rate of degeneration or decline; making the final point of degeneration less debilitating. In particularly preferred embodiments, the methods of the present invention can be to prevent or reduce the severity, or inhibit or minimise progression, of a sign or symptom of a disease or condition as described herein. As such, the methods of the present invention have utility as treatments as well as prophylaxes. As used herein, "preventing" or "prevention" is intended to refer to at least the reduction of likelihood of the risk of (or susceptibility to) acquiring a disease or disorder (i.e., causing at least one of the clinical signs or symptoms of the disease not to develop in an individual that may be exposed to or predisposed to the disease but does not yet experience or display signs or symptoms of the disease). Biological and physiological parameters for identifying such patients are provided herein and are also well known by physicians. Herein, the term “subject” or “patient" can be used interchangeably with each other. The term “individual” or “patient” refers to an animal that is treatable by the compound and / or method, respectively, including but not limited to, for example, dogs, cats, horses, sheep, pigs, cows, and the like, as well as human, non-human primates. Unless otherwise specified, the “subject” or “patient” may include both male and female genders. Further, it also includes a subject or patient, preferably a human, suitable for receiving treatment with a pharmaceutical composition and / or method of the present invention. The term "selective" means a greater activity against a first target (e.g., a 5-HT receptor subtype) relative to a second target (e.g., a second 5-HT receptor subtype). In some embodiments a compound has a selectivity of at least 1.25-fold, at least 1.5 fold, at least 2- fold, at least 3-fold, at least 4-fold, at least 5-fold, at least 6-fold, at least 10- fold or at least 100-fold greater towards a first target relative to a second target. In some embodiments, a compound described herein is selective towards the 5-HT2A receptor relative to one or more other 5-HT receptor subtypes such as 5-HT2B and / or 5-HT2C, preferably 5-HT2B. In some embodiments, a compound described herein is selective towards the 5-HT2c receptor relative to one or more other 5-HT receptor subtypes such as 5-HT2A and / or 5-HT2B, preferably 5-HT2B. "About" as used herein when referring to a measurable value such as an amount, a temporal duration, and the like, is meant to encompass variations of ±20% or ±10%, in some instances ±5%, in some instances ±1%, and in some instances ±0.1% from the specified value, as such variations are appropriate to perform the disclosed methods. Ranges: throughout this disclosure, various aspects of the invention can be presented in a range format. It should be understood that the description in range format is merely for convenience and brevity and should not be construed as an inflexible limitation on the scope of the invention. Accordingly, the description of a range should be considered to have specifically disclosed all the possible subranges as well as individual numerical values within that range. For example, description of a range such as from 1 to 6 should be considered to have specifically disclosed subranges such as from 1 to 3, from 1 to 4, from 1 to 5, from 2 to 4, from 2 to 6, from 3 to 6 etc., as well as individual numbers within that range, for example, 1, 2, 2.7, 3, 4, 5, 5.3, and 6. This applies regardless of the breadth of the range. As used herein the term "alkyl" refers to a straight or branched chain hydrocarbon radical having from one to twelve carbon atoms, or any range between, i.e. it contains 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 carbon atoms. The alkyl group is optionally substituted with substituents. Examples of "alkyl" as used herein include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, t-butyl, n-pentyl, isopentyl, and the like. As used herein, the terms "C1-C2alkyl", "C1-C3alkyl" and "C1-C6alkyl" refer to an alkyl group, as defined herein, containing at least 1, and at most 2, 3 or 6 carbon atoms respectively, or any range in between (eg alkyl groups containing 2-5 carbon atoms are also within the range of C1-C6). The term “alkylene” refers to a straight or branched, saturated, aliphatic radical having the number of carbon atoms indicated, and linking at least two other groups, i.e., a divalent hydrocarbon radical. The two moieties linked to the alkylene can be linked to the same atom or different atoms of the alkylene group. For instance, a straight chain alkylene can be the bivalent radical of –(CH2)n–, where n is 1, 2, 3, 4, 5 or 6. Representative alkylene groups include, but are not limited to, methylene, ethylene, propylene, isopropylene, butylene, isobutylene, sec-butylene, pentylene and hexylene. The term “alkenyl” whether it is used alone or as part of another group, means a straight or branched chain, saturated alkylene group, that is, a saturated carbon chain that contains substituents on two of its ends. The number of carbon atoms that are possible in the referenced alkylene group are indicated by the prefix “Cn1-n2”. For example, the term C2-6alkylene means an alkylene group having 2, 3, 4, 5 or 6 carbon atoms. Examples of alkenyl groups include, but are not limited to, vinyl (ethenyl), propenyl, isopropenyl, 1-butenyl, 2-butenyl, isobutenyl, butadienyl, 1-pentenyl, 2- pentenyl, isopentenyl, 1,3-pentadienyl, 1,4-pentadienyl, 1-hexenyl, 2-hexenyl, 3- hexenyl, 1,3-hexadienyl, 1 ,4-hexadienyl, 1,5-hexadienyl, 2,4-hexadienyl, or 1,3,5- hexatrienyl. The term “alkynyl” as used herein, whether it is used alone or as part of another group, means straight or branched chain, unsaturated alkynyl groups containing at least one triple bond. The number of carbon atoms that are possible in the referenced alkyl group are indicated by the prefix “Cn1-n2”. For example, the term C2-6alkynyl means an alkynyl group having 2, 3, 4, 5 or 6 carbon atoms. Examples of alkynyl groups include, but are not limited to, acetylenyl, propynyl, 1-butynyl, 2-butynyl, butadiynyl, 1-pentynyl, 2-pentynyl, isopentynyl, 1,3-pentadiynyl, 1,4-pentadiynyl, 1-hexynyl, 2-hexynyl, 3- hexynyl, 1,3-hexadiynyl, 1,4-hexadiynyl, 1,5-hexadiynyl, 2,4-hexadiynyl, or 1,3,5- hexatriynyl. The term "cycloalkyl" is intended to include mono-, bi- or tricyclic alkyl groups. The number of carbon atoms that are possible in the referenced cycloalkyl group are indicated by the prefix “Cn1-n2”. For example, the term C3-8cycloalkyl means an cycloalkyl group having 3, 4, 5, 6, 7 or 8 carbon atoms. In some embodiments, cycloalkyl groups have from 3 to 12, from 3 to 10, from 3 to 8, from 3 to 6, from 3 to 5 carbon atoms in the ring(s). In some embodiments, cycloalkyl groups have 5 or 6 ring carbon atoms. Examples of monocyclic cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl. In some embodiments, the cycloalkyl group has from 3 to 8, from 3 to 7, from 3 to 6, from 4 to 6, from 3 to 5, or from 4 to 5 ring carbon atoms. Bi- and tricyclic ring systems include bridged, spiro, and fused cycloalkyl ring systems. Examples of bi- and tricyclic ring cycloalkyl systems include, but are not limited to, bicyclo[2.1.1]hexanyl, bicyclo[2.2.1]heptanyl, adamantyl, and decalinyl. The term "alkylenecycloalkyl" refers to a radical having an alkyl component and a cycloalkyl component, where the alkyl component links the cycloalkyl component to the point of attachment· The alkyl component is as defined above, except that the alkyl component is at least divalent, an alkylene, to link to the cycloalkyl component and to the point of attachment. In some instances, the alkyl component can be absent. The alkyl component can include any number of carbons, such as C1-6, C1-2, C1-3, C1-4, C1-5, C2-3, C2-4, C2-5, C2-6, C3-4, C3-5, C3-6, C4-5, C4-6 and C5-6. The cycloalkyl component is as defined herein. The numerical range from x to y in “Cx-y alkylenecycloalkyl” relates to the total number of alkyl carbons and cycloalkyl ring atoms. Exemplary alkylenecycloalkyl groups include, but are not limited to, methylenecyclopropyl, methylenecyclobutyl, methylenecyclopentyl and methylenecyclohexyl. The term “aryl” refers to an aromatic ring system having any suitable number of ring atoms and any suitable number of rings. The number of carbon atoms that are possible in the referenced aryl group are indicated by the prefix “Cn1-n2”. For example, the term C6-12aryl means an aryl group having 6, 7, 8, 9, 10, 11 or 12 carbon atoms. Aryl groups can include any suitable number of ring atoms, such as, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 or 16 ring atoms, as well as from 6 to 10, 6 to 12, or 6 to 14 ring members. Aryl groups can be monocyclic, fused to form bicyclic or tricyclic groups, or linked by a bond to form a biaryl group. Representative aryl groups include phenyl, naphthyl and biphenyl. Other aryl groups include benzyl, having a methylene linking group. Some aryl groups have from 6 to 12 ring members, such as phenyl, naphthyl or biphenyl. Other aryl groups have from 6 to 10 ring members, such as phenyl or naphthyl. Some other aryl groups have 6 ring members, such as phenyl. The term “alkylenearyl” refers to a radical having an alkyl component and an aryl component, where the alkyl component links the aryl component to the point of attachment. The alkyl component is as defined above, except that the alkyl component is at least divalent, an alkylene, to link to the aryl component and to the point of attachment. The alkyl component can include any number of carbons, such as C1-6, C1- 2, C1-3, C1-4, C1-5, C1-6, C2-3, C2-4, C2-5, C2-6, C3-4, C3-5, C3-6, C4-5, C4-6 and C5-6. In some instances, the alkyl component can be absent. The aryl component is as defined above. The numerical range from x to y in “Cx-y alkylenearyl” relates to the total number of alkyl carbons and aryl ring atoms. Examples of alkylenearyl groups include, but are not limited to, benzyl and ethylenephenyl. As used herein, the term “alkoxy” refers to an alkyl group as defined herein covalently bound via an O linkage. The alkoxy group is optionally substituted with substituents. Examples of “alkoxy” as used herein include, but are not limited to methoxy, ethoxy, propoxy, isoproxy, butoxy, iso-butoxy, tert-butoxy and pentoxy. As used herein, the terms "C1-C2alkoxy", "C1-C3alkoxy" and "C1-C6alkoxy" refer to an alkoxy group, as defined herein, containing at least 1, and at most 2, 3 or 6 carbon atoms respectively, or any range in between (eg alkoxy groups containing 2-5 carbon atoms are also within the range of C1-C6). As used herein, the term “alkylamine” refers to an alkyl group as defined herein having one or more amino groups. The amino groups can be primary, secondary or tertiary. The alkyl amine can be further substituted with a hydroxy group to form an amino-hydroxy group. Examples of alkylamines include, but are not limited to, ethyl amine, propyl amine, isopropyl amine, ethylene diamine and ethanolamine. The amino group can link the alkyl amine to the point of attachment with the rest of the compound, be at the omega position of the alkyl group, or link together at least two carbon atoms of the alkyl group. As used herein, the terms "C1-C2alkylamine", "C1-C3alkylamine" and "C1-C6alkylamine " refer to an alkylamine group, as defined herein, containing at least 1, and at most 2, 3 or 6 carbon atoms respectively, or any range in between (e.g., alkylamine groups containing 2-5 carbon atoms are also within the range of C1-C6). As used herein, the term “alkylsulfonyl” refers to an alkyl group as defined herein having one or more sulfonyl groups. The sulfonyl group can link the alkylsulfonyl to the point of attachment with the rest of the compound, be at the omega position of the alkyl group, or link together at least two carbon atoms of the alkyl group. As used herein, the terms " C1-C2alkylsulfonyl", "C1-C3alkylsulfonyl" and "C1-C6alkylsulfonyl" refer to an alkylsulfonyl group, as defined herein, containing at least 1, and at most 2, 3 or 6 carbon atoms respectively, or any range in between (e.g., alkylsulfonyl groups containing 2-5 carbon atoms are also within the range of C1-C6). The term "heteroatom" as used herein means an atom of any element other than carbon or hydrogen. Examples of heteroatoms include nitrogen, oxygen, sulfur and phosphorus. Preferred heteroatoms include N, O and S, preferably N and O. The term “heteromoiety" as used herein means a chemical group comprising a heteroatom. Examples of heteromoieties include O, S, S(O), SO2, N and NH. A "substituent" as used herein, refers to a molecular moiety that is covalently bonded to an atom within a molecule of interest. Reference to “a substituent” may include a single substituent or to one or more substituents from the specified list. In some embodiments, a substituted moiety may include 1, 2, 3, 4, 5 or 6 substituents, preferably 1, 2, 3 or 4, more preferably 1, 2 or 3, 1 or 2 or only 1 substituent. For example, a "ring substituent" may be a moiety such as a halogen, alkyl group, or other substituent described herein that is covalently bonded to an atom, preferably a carbon or nitrogen atom, that is a ring member. The term "substituted," as used herein, means that any one or more hydrogens on the designated atom is replaced with a selection from the indicated substituents, provided that the designated atom's normal valence is not exceeded, and that the substitution results in a stable compound, ie, a compound that can be isolated, characterized and tested for biological activity. The terms "optionally substituted" or “may be substituted” and the like, as used throughout the specification, denotes that the group may or may not be further substituted or fused (so as to form a polycyclic system), with one or more non-hydrogen substituent groups. Suitable chemically viable substituents for a particular functional group will be apparent to those skilled in the art. Examples of substituents include but are not limited to C1-C6alkyl, C1-C6haloalkyl, C1-C6haloalkoxy, C1-C6hydroxyalkyl, C3-C7heterocyclyl, C3-C7cycloalkyl, C1- C6alkoxy, C1-C6alkylsulfanyl, C1-C6alkylsulfenyl, C1-C6alkylsulfonyl, C1-C6alkylsulfonylamino, arylsulfonoamino, alkylcarboxy, alkylcarboxyamide, oxo, hydroxy, mercapto, amino, acyl, carboxy, carbamoyl, aryl, aryloxy, heteroaryl, aminosulfonyl, aroyl, aroylamino, heteroaroyl, acyloxy, aroyloxy, heteroaroyloxy, alkoxycarbonyl, nitro, cyano, halo, ureido, C1-C6perfluoroalkyl. Preferably the substituents include amino, halo, C1-C6alkyl, amido, hydroxyl. As used herein, the term "halogen" refers to fluorine (F), chlorine (Cl), bromine (Br), or iodine (I) and the term "halo" refers to the halogen radicals fluoro (-F), chloro (- Cl), bromo (-Br), and iodo (-I). Preferably, ‘halo’ is fluoro or chloro. As used herein, the term “haloalkyl” refers to an alkyl group as defined herein in which one or more (up to all) of the available hydrogen atoms have been replacd with a halogen. In some instances, the term“perfluoro” can be used to define a compound or radical where all the hydrogens are replaced with fluorine. For example, perfluoromethyl refers to 1,1,1 -trifluoromethyl. As used herein, the terms "C1-C2haloalkyl", "C1-C3haloalkyl" and "C1-C6haloalkyl" refer to a haloalkyl group, as defined herein, containing at least 1, and at most 2, 3 or 6 carbon atoms respectively, or any range in between (e.g. haloalkyl groups containing 2-5 carbon atoms are also within the range of C1-C6). For example a C1haloalkyl group could be, but is not limited to, fluoromethyl, or difluoromethyl, or trifluoromethyl. As used herein, the term “haloalkenyl” refers to an alkenyl group as defined above in which one or more of the available hydrogen atoms have been replaced with a halogen. Thus, for example, “C1-6haloalkenyl” (or “C1-C6haloalkenyl”) refers to a C1to C6linear or branched alkenyl group as defined above with one or more halogen substituents. As used herein, the term “haloalkynyl” refers to an alkynyl group as defined above in which one or more of the available hydrogen atoms have been replaced with a halogen. Thus, for example, “C1-6haloalkynyl” (or “C1-C6haloalkynyl”) refers to a C1to C6linear or branched alkynyl group as defined above with one or more halogen substituents. As used herein the term haloalkoxy refers to an alkoxy group as defined herein substituted with at least one halogen. The term “amino” or “amine” refers to the group -NH2. The term “substituted amino” or “secondary amino” refers to an amino group having a hydrogen replaced with, for example a C1-C6alkyl group (“C1-C6alkylamino”), an aryl or aralkyl group (“arylamino”, “aralkylamino”) and so on. C1-C3alkylamino groups are preferred, such as for example, methylamino (NHMe), ethylamino (NHEt) and propylamino (NHPr). The term “disubstituted amino” or “tertiary amino” refers to an amino group having the two hydrogens replaced with, for example aC1-C6alkyl group, which may be the same or different (“dialkylamino”), an aryl and alkyl group (“aryl(alkyl)amino”) and so on. Di(C1-C3alkyl)amino groups are preferred, such as for example, dimethylamino (NMe2), diethylamino (NEt2), dipropylamino (NPr2) and variations thereof (eg N(Me)(Et) and so on). The term “nitro” refers to the group – NO2. The term “cyano” and “nitrile” refer to the group –CN. The term “amido” or “amide” refers to the group -C(O)NH2. The term “substituted amido” or “substituted amide” refers to an amido group having a hydrogen replaced with, for example a C1-C6alkyl group (“C1-C6alkylamido” or “C1-C6alkylamide”), an aryl (“arylamido”), aralkyl group (“aralkylamido”) and so on. C1- C3alkylamide groups are preferred, such as for example, methylamide (-C(O)NHMe), ethylamide (-C(O)NHEt) and propylamide (-C(O)NHPr) and includes reverse amides thereof (eg NHMeC(O)-, -NHEtC(O)- and –NHPrC(O)-). The term “disubstituted amido” or “disubstituted amide” refers to an amido group having the two hydrogens replaced with, for example a C1-C6alkyl group (“di(C1-C6alkyl)amido” or “di(C1-C6alkyl)amide”), an aralkyl and alkyl group (“alkyl(aralkyl)amido”) and so on. Di(C1-C3alkyl)amide groups are preferred, such as for example, dimethylamide (-C(O)NMe2), diethylamide (-C(O)NEt2) and dipropylamide ((-C(O)NPr2) and variations thereof (eg C(O)N(Me)Et and so on) and includes reverse amides thereof. The term “sulfonyl” refers to the group -SO2H. The term “substituted sulfonyl” refers to a sulfonyl group having the hydrogen replaced with, for example a C1-C6alkyl group (“sulfonylC1-C6alkyl”), an aryl (“arylsulfonyl”), an aralkyl (“aralkylsulfonyl”) and so on. Sulfonyl C1-C3alkyl groups are preferred, such as for example, -SO2Me, -SO2Et and -SO2Pr. The term “sulfonylamido” or “sulfonamide” refers to the group -SO2NH2. The term “substituted sulfonamido” or “substituted sulphonamide” refers to an sulfonylamido group having a hydrogen replaced with, for example a C1-C6alkyl group (“sulfonylamidoC1-C6alkyl”), an aryl (“arylsulfonamide”), aralkyl (“aralkylsulfonamide”) and so on. SulfonylamidoC1-C3alkyl groups are preferred, such as for example, SO2NHMe, SO2NHEt and -SO2NHPr and includes reverse sulfonamides thereof (e.g. - NHSO2Me, NHSO2Et and -NHSO2Pr). The term “disubstituted sufonamido” or “disubstituted sulphonamide” refers to an sulfonylamido group having the two hydrogens replaced with, for example a C1-C6alkyl group, which may be the same or different (“sulfonylamidodi(C1-C6alkyl)”), an aralkyl and alkyl group (“sulfonamido(aralkyl)alkyl”) and so on. Sulfonylamidodi(C1-C3alkyl) groups are preferred, such as for example, -SO2NMe2, -SO2NEt2 and -SO2NPr2and variations thereof (eg SO2N(Me)Et and so on) and includes reserve sulfonamides thereof (eg –N(Me)SO2Me and so on). The term “sulfate” refers to the group OS(O)2OH and includes groups having the hydrogen replaced with, for example a C1-C6alkyl group (“alkylsulfates”), an aryl (“arylsulfate”), an aralkyl (“aralkylsulfate”) and so on. C1-C3alkylsulfates are preferred, such as for example, OS(O)2OMe, OS(O)2OEt and OS(O)2OPr. The term “sulfonate” refers to the group SO3H and includes groups having the hydrogen replaced with, for example a C1-C6alkyl group (“alkylsulfonate”), an aryl (“arylsulfonate”), an aralkyl (“aralkylsulfonate”) and so on. C1-C3alkylsulfonates are preferred, such as for example, SO3Me, SO3Et and SO3Pr. The term “amino acid” as herein defined refers to a moiety containing an amino group and a carboxyl group linked by at least one carbon. An amino acid may refer a natural or non-natural amino acid, preferably a natural amino acid such as alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glutamine, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine, valine, preferably the amino acid is arginine, lysine or histidine, most preferably lysine. The term “carboxylate” or “carboxyl” refers to the group -COO- or -COOH. The term “carbamate” refers to the group –OC(O)NH2. The carbamate may be substituted, or may be disubstituted, for example with an alkyl group such as but not limited to C1-C6alkyl. The term “carbonate” refers to the group –OC(O)O- or –OC(O)OH. The term “alkylcarbonate” as herein defined refers to a carbonate group having the hydrogen replaced with, for example a C1-C6alkyl group, an aryl or aralkyl group (“arylcarbonate” or “aralkylcarbonate”) and so on. CO3C1-C3alkyl groups are preferred, such as for example, methylcarbonate (CO3Me), ethylcarbonate (CO3Et) and propylcarbonate (CO3Pr). The term “ester” refers to a carboxyl group having the hydrogen replaced with, for example a C1-C6alkyl group (“carboxylC1-C6alkyl” or “alkylester”), an aryl or aralkyl group (“arylester” or “aralkylester”) and so on. CO2C1-C3alkyl groups are preferred, such as for example, methylester (CO2Me), ethylester (CO2Et) and propylester (CO2Pr) and includes reverse esters thereof (eg –OC(O)Me, -OC(O)Et and –OC(O)Pr). The term “heterocyclyl” refers to a moiety obtained by removing a hydrogen atom from a ring atom of a heterocyclic compound which moiety has from 3 to 12 ring atoms (unless otherwise specified), of which 1, 2, 3, 4 or more are ring heteroatoms, for example independently selected from O, S and N, or ring heteromoieties, for example independently selected from O, S, S(O), SO2, N and NH. When a heterocyclyl group contains the prefix Cn1-n2 or “n1 to n2” this prefix indicates the number of carbon atoms in the corresponding carbocyclic group, in which one or more, suitably 1, 2, 3, 4 or more, of the ring atoms is replaced with a heteroatom or heteromoiety. In this context, the prefixs 3-, 4-, 5-, 6-, 7-, 8-, 9- and 10- membered denote the number of ring atoms, or range of ring atoms, whether carbon atoms or heteroatoms. For example, the term “C3-10 heterocyclyl” or “3-10 membered heterocylyl”, as used herein, pertains to a heterocyclyl group having 3, 4, 5, 6, 7, 8, 9 or 10 ring atoms. Examples of heterocylyl groups include 5-6-membered monocyclic heterocyclyls and 9- 10 membered fused bicyclic heterocyclyls. Examples of monocyclic heterocyclyl groups include, but are not limited to, those containing one nitrogen atom such as aziridine (3-membered ring), azetidine (4- membered ring), pyrrolidine (tetrahydropyrrole), pyrroline (eg 3-pyrroline, 2,5- dihydropyrrole), 2Hpyrrole or 3H-pyrrole (isopyrrole, isoazole) or pyrrolidinone (5- membered rings), piperidine, dihydropyridine, tetrahydropyridine (6-membered rings), and azepine (7membered ring); those containing two nitrogen atoms such as imidazoline, pyrazolidine (diazolidine), imidazoline, pyrazoline (dihydropyrazole) (5- membered rings), piperazine (6membered ring); those containing one oxygen atom such as oxirane (3-membered ring), oxetane (4-membered ring), oxolane (tetrahydrofuran), oxole (dihydrofuran) (5-membered rings), oxane (tetrahydropyran), dihydropyran, pyran (6-membered rings), oxepin (7membered ring); those containing two oxygen atoms such as dioxolane (5-membered ring), dioxane (6-membered ring), and dioxepane (7-membered ring); those containing three oxygen atoms such as trioxane (6-membered ring); those containing one sulfur atom such as thiirane (3- membered ring), thietane (4-membered ring), thiolane (tetrahydrothiophene) (5- membered ring), thiane (tetrahydrothiopyran) (6-membered ring), thiepane (7- membered ring); those containing one nitrogen and one oxygen atom such as tetrahydrooxazole, dihydrooxazole, tetrahydroisoxazole, dihydroisoxazole (5-membered rings), morpholine, tetrahydrooxazine, dihydrooxazine, oxazine (6-membered rings); those containing one nitrogen and one sulfur atom such as thiazoline, thiazolidine (5- membered rings), thiomorpholine (6-membered ring); those containing two nitrogen and one oxygen atom such as oxadiazine (6-membered ring); those containing one oxygen and one sulfur such as: oxathiole (5-membered ring) and oxathiane (thioxane) (6- membered ring); and those containing one nitrogen, one oxygen and one sulfur atom such as oxathiazine (6-membered ring). Heterocyclyls also encompass heteroaryl (aromatic heterocyclyls) and heterocycloalkyl (non-aromatic heterocyclyls). Such groups may be substituted or unsubstituted. The term “aromatic heterocyclyl” may be used interchangeably with the term “heteroaromatic” or the term “heteroaryl” or “hetaryl”. The heteroatoms in the aromatic heterocyclyl group may be independently selected from N, S and O. The aromatic heterocyclyl groups may comprise 1, 2, 3, 4 or more ring heteroatoms. When a heteroaryl group contains the prefix Cn1-n2 or “n1 to n2” this prefix indicates the number of carbon atoms in the corresponding aryl group, in which one or more, suitably 1, 2, 3, 4 or more, of the ring atoms is replaced with a heteroatom. In the case of fused aromatic heterocyclyl groups, only one of the rings may contain a heteroatom and not all rings must be aromatic. “Heteroaryl” is used herein to denote a heterocyclic group having aromatic character and embraces aromatic monocyclic ring systems and polycyclic (eg bicyclic) ring systems containing one or more aromatic rings. The term aromatic heterocyclyl also encompasses pseudoaromatic heterocyclyls. The term “pseudoaromatic” refers to a ring system which is not strictly aromatic, but which is stabilized by means of delocalization of electrons and behaves in a similar manner to aromatic rings. The term aromatic heterocyclyl therefore covers polycyclic ring systems in which all of the fused rings are aromatic as well as ring systems where one or more rings are non-aromatic, provided that at least one ring is aromatic. In polycyclic systems containing both aromatic and non-aromatic rings fused together, the group may be attached to another moiety by the aromatic ring or by a non-aromatic ring. Examples of heteroaryl groups are monocyclic and bicyclic groups containing from five to ten ring members. The heteroaryl group can be, for example, a five membered or six membered monocyclic ring or a bicyclic structure formed from fused five and six membered rings or two fused six membered rings or two fused five membered rings. Each ring may contain up to about four heteroatoms typically selected from nitrogen, sulphur and oxygen. The heteroaryl ring will contain up to 4 heteroatoms, more typically up to 3 heteroatoms, more usually up to 2, for example a single heteroatom. In one embodiment, the heteroaryl ring contains at least one ring nitrogen atom. The nitrogen atoms in the heteroaryl rings can be basic, as in the case of an imidazole or pyridine, or essentially non-basic as in the case of an indole or pyrrole nitrogen. In general the number of basic nitrogen atoms present in the heteroaryl group, including any amino group substituents of the ring, will be less than five. Aromatic heterocyclyl groups may be 5-membered or 6-membered mono-cyclic aromatic ring systems. Examples of 5-membered monocyclic heteroaryl groups include but are not limited to furanyl, thienyl, pyrrolyl, oxazolyl, oxadiazolyl (including 1,2,3 and 1,2,4 oxadiazolyls and furazanyl i.e.1,2,5-oxadiazolyl), thiazolyl, isoxazolyl, isothiazolyl, pyrazolyl, imidazolyl, triazolyl (including 1,2,3, 1,2,4 and 1,3,4 triazolyls), oxatriazolyl, tetrazolyl, thiadiazolyl (including 1,2,3 and 1,3,4 thiadiazolyls) and the like. Examples of 6-membered monocyclic heteroaryl groups include but are not limited to pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, pyranyl, oxazinyl, dioxinyl, thiazinyl, thiadiazinyl and the like. Examples of 6-membered aromatic heterocyclyls containing nitrogen include pyridyl (1 nitrogen), pyrazinyl, pyrimidinyl and pyridazinyl (2 nitrogens). Aromatic heterocyclyl groups may also be bicyclic or polycyclic heteroaromatic ring systems such as fused ring systems (including purine, pteridinyl, napthyridinyl, 1H thieno[2,3-c]pyrazolyl, thieno[2,3-b]furyl and the like) or linked ring systems (such as oligothiophene, polypyrrole and the like). Fused ring systems may also include aromatic 5-membered or 6-membered heterocyclyls fused to carbocyclic aromatic rings such as phenyl, napthyl, indenyl, azulenyl, fluorenyl, anthracenyl and the like, such as 5- membered aromatic heterocyclyls containing nitrogen fused to phenyl rings, 5- membered aromatic heterocyclyls containing 1 or 2 nitrogens fused to phenyl ring. A bicyclic heteroaryl group may be, for example, a group selected from: a) a benzene ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms; b) a pyridine ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms; c) a pyrimidine ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; d) a pyrrole ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms; e) a pyrazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; f) an imidazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; g) an oxazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; h) an isoxazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; i) a thiazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; j) an isothiazole ring fused to a 5- or 6-membered ring containing 1 or 2 ring heteroatoms; k) a thiophene ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms; I) a furan ring fused to a 5- or 6membered ring containing 1, 2 or 3 ring heteroatoms; m) a cyclohexyl ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms; and n) a cyclopentyl ring fused to a 5- or 6-membered ring containing 1, 2 or 3 ring heteroatoms. Particular examples of bicyclic heteroaryl groups containing a five membered ring fused to another five membered ring include but are not limited to imidazothiazole (e.g. imidazo[2,1-b]thiazole) and imidazoimidazole (e.g. imidazo[1,2-a]imidazole). Particular examples of bicyclic heteroaryl groups containing a six membered ring fused to a five membered ring include but are not limited to benzofuran, benzothiophene, benzimidazole, benzoxazole, isobenzoxazole, benzisoxazole, benzothiazole, benzisothiazole, isobenzofuran, indole, isoindole, indolizine, indoline, isoindoline, purine (e.g., adenine, guanine), indazole, pyrazolopyrimidine (e.g. pyrazolo[1 ,5-a]pyrimidine), benzodioxole and pyrazolopyridine (e.g. pyrazolo[1,5- a]pyridine) groups. A further example of a six membered ring fused to a five membered ring is a pyrrolopyridine group such as a pyrrolo[2,3-b]pyridine group. Particular examples of bicyclic heteroaryl groups containing two fused six membered rings include but are not limited to quinoline, isoquinoline, chroman, thiochroman, chromene, isochromene, isochroman, benzodioxan, quinolizine, benzoxazine, benzodiazine, pyridopyridine, quinoxaline, quinazoline, cinnoline, phthalazine, naphthyridine and pteridine groups. Examples of heteroaryl groups containing an aromatic ring and a non-aromatic ring include tetrahydronaphthalene, tetrahydroisoquinoline, tetrahydroquinoline, dihydrobenzothiophene, dihydrobenzofuran, 2,3-dihydro- benzo[1,4]dioxine, benzo[1,3]dioxole, 4,5,6,7-tetrahydrobenzofuran, indoiine, isoindoline and indane groups. Examples of aromatic heterocyclyls fused to carbocyclic aromatic rings may therefore include but are not limited to benzothiophenyl, indolyl, isoindolyl, benzofuranyl, isobenzofuranyl, benzimidazolyl, indazolyl, benzoxazolyl, benzisoxazolyl, isobenzoxazoyl, benzothiazolyl, benzisothiazolyl, quinolinyl, isoquinolinyl, quinoxalinyl, quinazolinyl, cinnolinyl, benzotriazinyl, phthalazinyl, carbolinyl and the like. The term “heterocycloalkyl” or “non-aromatic heterocyclyl” encompasses optionally substituted saturated and unsaturated rings which contain at least one heteroatom such as N, S and O, or a heteromoiety such as O, S, S(O), SO2, N and NH. The ring may contain 1, 2, 3, 4 or more heteroatoms or heteromoieties. When a heterocycloalkyl group contains the prefix Cn1-n2 or “n1 to n2” this prefix indicates the number of carbon atoms in the corresponding carbocyclic group, in which one or more, suitably 1, 2, 3, 4 or more, of the ring atoms is replaced with a heteroatom or heteromoiety. The ring may be a monocyclic ring or part of a polycyclic ring system. Polycyclic ring systems include fused rings and spirocycles. Not every ring in a non- aromatic heterocyclic polycyclic ring system must contain a heteroatom, provided at least one ring contains one or more heteroatoms. Non-aromatic heterocyclyls may be 3-8 membered mono-cyclic rings. Examples of 5-membered non-aromatic heterocyclyl rings include 2H-pyrrolyl, 1pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrrolidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3- pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrazolinyl, 2-pyrazolinyl, 3- pyrazolinyl, pyrazolidinyl, 2-pyrazolidinyl, 3-pyrazolidinyl, imidazolidinyl, 3-dioxalanyl, thiazolidinyl, isoxazolidinyl, 2-imidazolinyl and the like. Examples of 6-membered non-aromatic heterocyclyls include piperidinyl, piperidinonyl, pyranyl, dihyrdopyranyl, tetrahydropyranyl, 2H pyranyl, 4H pyranyl, thianyl, thianyl oxide, thianyl dioxide, piperazinyl, diozanyl, 1,4-dioxinyl, 1,4-dithianyl, 1,3,5triozalanyl, 1,3,5-trithianyl, 1,4-morpholinyl, thiomorpholinyl, 1,4-oxathianyl, triazinyl, 1,4thiazinyl and the like. Examples of 7-membered non-aromatic heterocyclyls include azepanyl, oxepanyl, thiepanyl and the like. Non-aromatic heterocyclyl rings may also be bicyclic heterocyclyl rings such as linked ring systems (for example uridinyl and the like) or fused ring systems. Fused ring systems include non-aromatic 5-membered, 6-membered or 7-membered heterocyclyls fused to carbocyclic aromatic rings such as phenyl, napthyl, indenyl, azulenyl, fluorenyl, anthracenyl and the like. Examples of non-aromatic 5-membered, 6-membered or 7membered heterocyclyls fused to carbocyclic aromatic rings include indolinyl, benzodiazepinyl, benzazepinyl, dihydrobenzofuranyl and the like. The term “alkyleneheteroaryl” refers to a radical having an alkyl component and a heteroaryl component, where the alkyl component links the heteroaryl component to the point of attachment· The alkyl component is as defined above, except that the alkyl component is at least divalent, an alkylene, to link to the heteroaryl component and to the point of attachment. In some instances, the alkyl component can be absent. The alkyl component can include any number of carbons, such as C1-6, C1-2, C1-3, C1-4, C1-5, C2-3, C2-4, C2-5, C2-6, C3-4, C3-5, C3-6, C4-5, C4-6 and C5-6. The heteroaryl component is as defined herein. The numerical range from x to y in “Cx-y alkylenecycloalkyl” relates to the total number of alkyl carbons and heteroaryl ring atoms (carbon and heteroatoms together). The term “alkyleneheterocycloalkyl” refers to a radical having an alkyl component and a heterocycloalkyl component, where the alkyl component links the heterocycloalkyl component to the point of attachment· The alkyl component is as defined above, except that the alkyl component is at least divalent, an alkylene, to link to the heterocycloalkyl component and to the point of attachment. In some instances, the alkyl component can be absent. The alkyl component can include any number of carbons, such as C1-6, C1-2, C1-3, C1-4, C1-5, C2-3, C2-4, C2-5, C2-6, C3-4, C3-5, C3-6, C4-5, C4-6 and C5-6. The heterocycloalkyl component is as defined herein. The numerical range from x to y in “Cx- y alkyleneheterocycloalkyl” relates to the total number of alkyl carbons and heterocycloalkyl ring atoms (carbon and heteroatoms together). As used herein, the term solvate refers to a complex of the compound and either stoichiometric or non-stoichiometric amounts of a solvent. Solvates are often formed during the process of crystallization with pharmaceutically acceptable solvents such as water, ethanol, and the like. Hydrates are formed when the solvent is water, or alcoholates are formed when the solvent is alcohol. As used herein, the term polymorph refers to the different crystal packing arrangements of the same elemental composition of a compound. Polymorphs usually have different X-ray diffraction patterns, infrared spectra, melting points, density, hardness, crystal shape, optical and electrical properties, stability, and solubility. Various factors such as the recrystallization solvent, rate of crystallization, and storage temperature may cause a single crystal form to dominate. As used herein, the term “metabolite” refers to a derivative of a compound that is formed when the compound is metabolized. The term "active metabolite" refers to a biologically active derivative of a compound that is formed when the compound is metabolized. The term "metabolized," as used herein, refers to the sum of the processes (including, but not limited to, hydrolysis reactions and reactions catalyzed by enzymes) by which a particular substance is changed by an organism. Thus, enzymes may produce specific structural alterations to a compound. Metabolites of the compounds disclosed herein are optionally identified either by administration of compounds to a host and analysis of tissue samples from the host, or by incubation of compounds with hepatic cells in vitro and analysis of the resulting compounds. Stereochemical definitions and conventions used herein generally follow S. P. Parker, Ed., McGraw-Hill Dictionary of Chemical Terms (1984) McGraw-Hill Book Company, New York; and Eliel, E. and Wilen, S., “Stereochemistry of Organic Compounds”, John Wiley & Sons, Inc., New York, 1994. The compounds of the invention may contain asymmetric or chiral centers, and therefore exist in different stereoisomeric forms. The term “stereoisomers” refers to compounds which have identical chemical constitution, but differ with regard to the arrangement of the atoms or groups in space. As used herein, the term “stereoisomer” includes but is not limited to diastereomers, enantiomers and atropisomers, as well as mixtures thereof such as racemic mixtures. As used herein, the term "pharmaceutically acceptable salt" refers to those salts which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of humans and lower animals without undue toxicity, irritation, allergic response and the like, and are commensurate with a reasonable benefit / risk ratio. Pharmaceutically acceptable salts are well known in the art. For example, S. M. Berge et al., describe pharmaceutically acceptable salts in detail in J. Pharmaceutical Sciences, 1977, 66, 1–19, incorporated herein by reference. Pharmaceutically acceptable salts of the compounds of this invention include those derived from suitable inorganic and organic acids and bases. Examples of pharmaceutically acceptable, nontoxic acid addition salts are salts of an amino group formed with inorganic acids such as hydrochloric acid, hydrobromic acid, phosphoric acid, sulfuric acid and perchloric acid or with organic acids such as acetic acid, oxalic acid, maleic acid, tartaric acid, citric acid, succinic acid or malonic acid or by using other methods used in the art such as ion exchange. Other pharmaceutically acceptable salts include adipate, alginate, ascorbate, aspartate, benzenesulfonate, benzoate, bisulfate, borate, butyrate, camphorate, camphorsulfonate, citrate, cyclopentanepropionate, digluconate, dodecylsulfate, ethanesulfonate, formate, fumarate, glucoheptonate, glycerophosphate, gluconate, hemisulfate, heptanoate, hexanoate, hydroiodide, 2–hydroxy– ethanesulfonate, lactobionate, lactate, laurate, lauryl sulfate, malate, maleate, malonate, methanesulfonate, 2–naphthalenesulfonate, nicotinate, nitrate, oleate, oxalate, palmitate, pamoate, pectinate, persulfate, 3–phenylpropionate, phosphate, pivalate, propionate, stearate, succinate, sulfate, tartrate, thiocyanate, p–toluenesulfonate, undecanoate, valerate salts, and the like. Compounds The present disclosure provides compounds of formula (I): or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein L is selected from C1-4 alkylene, C2-4 alkenylene and C2-4 alkynylene; R1is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5- 10 heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14alkylenecycloalkyl, C3-C8heterocycloalkyl, C4- C14 alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R2is independently selected from hydrogen, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; alternatively R1and R2together with the atoms to which they are attached form a C3-8heterocycloalkyl including 0, 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR11, said C3-8heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-8alkylamino, C1-8alkylsulfonyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R3is selected from hydrogen, C1-6alkyl, C3-8cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R3and one of R1and R2together with the atoms to which they are attached form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; each R11is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl, and C3-7heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl and C3-7heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R12, C(O)N(R12)2, OR12, N(R12)2, NO2, SR12and SO2R12, said C3-C7cycloalkyl and C3-7heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12; each R12is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, CN, OR13, N(R13)2, SR13, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, C4-16alkyleneheteroaryl; said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13and SO2R13, said C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4- 16 alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12 aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein at least one of R4, R5, R6and R8is other than hydrogen. In some embodiments, the compound is not selected from one or more of the group consisting of: or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, or polymorph thereof. In some embodiments, when R4is OH or OMe; then R1and R2are not both hydrogen. In some embodiments, when R4is fluoro; then R1and R2are not both hydrogen. In some embodiments, when R5is OMe; then R1and R2are not both hydrogen. In some embodiments, when R5is fluoro; then R1and R2are not both hydrogen. In some embodiments, when R6is OH or OMe; then i) R1and R2are not both hydrogen, and / or ii) R1and R2are not both C2alkyl. In some embodiments, when R6is fluoro; then i) R1and R2are not both hydrogen, and / or ii) if one of R1and R2is hydrogen then the other one of R1and R2is not C2alkyl. In some embodiments, when R6is chloro; then i) R1and R2are not both hydrogen, and / or ii) if one of R1and R2is hydrogen then the other one of R1and R2is not C2alkyl. In some embodiments, when R6is bromo; then if one of R1and R2is hydrogen then the other one of R1and R2is not C2alkyl. In some embodiments, when R6is OMe; then i) if one of R1and R2is hydrogen then the other one of R1and R2is not C1alkyl, iso-propyl, sec-butyl or tert-butyl; and / or ii) R1and R2are not both hydrogen. In some embodiments, when R6is bromo; then i) R1and R2are not both hydrogen, and / or ii) if one of R1and R2is hydrogen then the other one of R1and R2is not C1alkyl. In some embodiments, when R6is fluoro; then if one of R1and R2is hydrogen then the other one of R1and R2is not C1alkyl. In some embodiments, when R6is chloro; then if one of R1and R2is hydrogen then the other one of R1and R2is not C1alkyl. In some embodiments, when R6is OMe; then if one of R1and R2is hydrogen then the other one of R1and R2is not C2-4alkyl. In some embodiments, when R8is OMe or OH; then R1and R2are not both hydrogen. In some embodiments, when R8is OMe; then R1and R2are not both C1alkyl. In some embodiments, when R8is OMe; then R1and R2are not both C1-6alkyl. In some embodiments, when R8is OMe; then R1and R2are not both C1-2alkyl. In some embodiments, when R8is OMe; then R1and R2are not both C1alkyl. In some embodiments, when R8is fluoro; then i) R1and R2are not both hydrogen, and / or ii) if one of R1and R2is hydrogen then the other one of R1and R2is not C1alkyl. L In some embodiments, L is C1-4 alkylene. In some embodiments, L is methylene. R4, R5, R6and R8In some embodiments, only one of R4, R5, R6and R8is other than hydrogen. In some embodiments, R4is other than hydrogen. In some embodiments, R4is other than hydrogen and R5-R10are hydrogen. In some embodiments, R5is other than hydrogen. In some embodiments, R5is other than hydrogen and R4and R6-R10are hydrogen. In some embodiments, R6is other than hydrogen. In some embodiments, R6is other than hydrogen and R4-R5and R7-R10are hydrogen. In some embodiments, R8is other than hydrogen. In some embodiments, R8is other than hydrogen and R4-R7and R9-R10are hydrogen. In some embodiments, R4is selected from halogen, CN, OR13, N(R13)2, SR13, C1- 6 alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1- 6 alkylamine, C1-6alkoxy, C1-6haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, C4-16alkyleneheteroaryl; said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13and SO2R13, said C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; and R5, R6and R8are each H. In some embodiments, R4is selected from halogen (eg F), -OH and optionally substituted C1-6alkoxy (eg methoxy), and R5, R6and R8are each H. In some embodiments, R4is selected from F, -OH and optionally substituted methoxy, and R5, R6and R8are each H. In some embodiments, R5is selected from halogen, CN, OR13, N(R13)2, SR13, C1- 6 alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1- 6 alkylamine, C1-6alkoxy, C1-6haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, C4-16alkyleneheteroaryl; said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13and SO2R13, said C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4- 16 alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; and R4, R6and R8are each H. In some embodiments, R5is selected from halogen (eg F), -OH and optionally substituted C1-6alkoxy (eg methoxy), and R4, R6and R8are each H. In some embodiments, R5is selected from F, -OH and optionally substituted methoxy, and R5, R6and R8are each H. In some embodiments, R6is selected from halogen, CN, OR13, N(R13)2, SR13, C1- 6 alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1- 6 alkylamine, C1-6alkoxy, C1-6haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8cycloalkyl, C3-14alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, C4-16alkyleneheteroaryl; said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13and SO2R13, said C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4- 16 alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; and R4, R5and R8are each H. In some embodiments, R6is selected from halogen (eg F), -OH and optionally substituted C1-6alkoxy (eg methoxy), and R4, R5and R8are each H. In some embodiments, R6is selected from F, -OH and optionally substituted methoxy, and R4, R5and R8are each H. In some embodiments, R8is selected from halogen, CN, OR13, N(R13)2, SR13, C1- 6 alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1- 6 alkylamine, C1-6alkoxy, C1-6haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, C4-16alkyleneheteroaryl; said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13and SO2R13, said C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4- 16 alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; and R4, R5and R6are each H. In some embodiments, R8is selected from halogen (eg F), -OH and optionally substituted C1-6alkoxy (eg methoxy), and R4, R5and R6are each H. In some embodiments, R8is selected from F, -OH and optionally substituted methoxy, and R4, R5and R6are each H. R1and R2In some embodiments, R1and R2are each independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl. In some embodiments, R1and R2are each independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl and C7-18alkylenearyl. In some embodiments, R1and R2are each independently selected from hydrogen, C1-4 alkyl, C1-4 haloalkyl, C3-4 cycloalkyl, C4-5 alkylenecycloalkyl, and C7alkylenearyl. In some embodiments, R1and R2are each independently selected from C1-4 alkyl, C1-4 haloalkyl, C3-4 cycloalkyl, C4-5 alkylenecycloalkyl, and C7alkylenearyl. In some embodiments, R1and R2are each independently selected from hydrogen, C1-4alkyl and C1-4haloalkyl; preferably hydrogen and C1-4alkyl. In some embodiments, R1and R2are each independently selected from C1-4 alkyl. In some embodiments, R1and R2are each independently selected from hydrogen, C4-5 alkylenecycloalkyl, and C7alkylenearyl. In some embodiments, R1and R2are each independently selected from C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl and C4-14 alkylenecycloalkyl. In some embodiments, both of R1and R2are the same. In some embodiments, each of R1and R2are different. In some embodiments, one of R1and R2is unsubstituted. In some embodiments, both of R1and R2are unsubstituted. In some embodiments, at least one of the alkyl groups at R1and R2are linear. In some embodiments, both of the alkyl groups at R1and R2are linear. In some embodiments, at least one of the alkyl groups at R1and R2are branched. In some embodiments, at least one of R1and R2is not C1-6alkyl. In some embodiments, both of R1and R2are not C1-6alkyl. In some embodiments, at least one of R1and R2is C1-6alkyl. In some embodiments, both of R1and R2are C1-6alkyl. In some embodiments, at least one of R1and R2is not C3-8cycloalkyl. In some embodiments, both of R1and R2are not C3-8cycloalkyl. In some embodiments, at least one of R1and R2is C3-8cycloalkyl. In some embodiments, at least one of R1and R2is not C4-14 alkylenecycloalkyl. In some embodiments, both of R1and R2are not C4-14 alkylenecycloalkyl. In some embodiments, at least one of R1and R2is C4-14 alkylenecycloalkyl. In some embodiments, at least one of R1and R2is not C1alkyl. In some embodiments, both of R1and R2are not C1alkyl. In some embodiments, at least one of R1and R2is C1alkyl. In some embodiments, both of R1and R2are C1alkyl. In some embodiments, at least one of R1and R2is not C2alkyl. In some embodiments, both of R1and R2are not C2alkyl. In some embodiments, at least one of R1and R2is C2alkyl. In some embodiments, at least one of R1and R2is not C3alkyl. In some embodiments, both of R1and R2are not C3alkyl. In some embodiments, at least one of R1and R2is C3alkyl. In some embodiments, at least one of R1and R2is not hydrogen. In some embodiments, both of R1and R2are not hydrogen. In some embodiments, at least one of R1and R2is hydrogen. In some embodiments, both of R1and R2are hydrogen. In some embodiments, one of R1and R2is hydrogen and the other one is C1-6alkyl. In some embodiments, one of R1and R2is hydrogen and the other one is not C1-6alkyl. In some embodiments, one of R1and R2is C1-6alkyl and the other one is not hydrogen. In some embodiments, one of R1and R2is hydrogen and the other one is not C3- 8 cycloalkyl. In some embodiments, one of R1and R2is C3-8cycloalkyl and the other one is not hydrogen. In some embodiments, one of R1and R2is hydrogen and the other one is C4-14 alkylenecycloalkyl. In some embodiments, one of R1and R2is hydrogen and the other one is not C4-14 alkylenecycloalkyl. In some embodiments, one of R1and R2is C4-14 alkylenecycloalkyl and the other one is not C1-6alkyl. In some embodiments, one of R1and R2is C1-6alkyl and the other one is C3-8cycloalkyl. In some embodiments, one of R1and R2is C1-6alkyl and the other one is not C3-8cycloalkyl. In some embodiments, R1and R2, together with the nitrogen to which they are attached, form any one of the following:

[0009] . In some embodiments, R1and R2together with the nitrogen to which they are attached form any one of the following: In some embodiments, R1and R2together with the nitrogen to which they are attached form any one of the following: In some embodiments, R1and R2together with the nitrogen to which they are attached form any one of the following: In some embodiments, R1and R2together with the nitrogen to which they are attached form any one of the following: . In some embodiments, R1and R2together with the atoms to which they are attached form a C3-8heterocycloalkyl including 0, 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR11. In some embodiments, R1and R2together with the atoms to which they are attached form a C4-5 heterocycloalkyl including 0, 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR11. In some embodiments, the heterocyclyl formed by R1and R2combined with the atoms to which they are attached to does not include any additional ring heteromoieties. In some embodiments, the heterocyclyl formed by R1and R2combined with the atoms to which they are attached, is unsubstituted. R3, R1& R2In some embodiments, R3is hydrogen. In some embodiments, R3and one of R1and R2together with the atoms to which they are attached form a C3-8heterocycloalkyl, said C3-8heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11, wherein R11is as defined herein. R4to R10Each of R4, R5, R6, R7, R8, R9and R10may be the same or different. Preferably, only one of R4, R5, R6, R7, R8, R9and R10is other than H. In some embodiments, R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, OR13, C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, C2-4 haloalkenyl, C2-4 alkynyl, C2-4 haloalkynyl, C1-4 alkylamine, C1-4 alkoxy and C1-4 haloalkoxy. In some embodiments, R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, OR13, C1-2 alkyl, C1-2 haloalkyl, C1-2 alkoxy and C1-2 haloalkoxy. In some embodiments, R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, OR13, and C1-2 alkyl; preferably hydrogen, halogen and OR13; more preferably hydrogen, fluoro and OR13. In some embodiments, R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen and OR13. In some embodiments, R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, OH, C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, C2-4 haloalkenyl, C2-4 alkynyl, C2-4 haloalkynyl, C1-4 alkylamine, C1-4 alkoxy and C1-4 haloalkoxy. In some embodiments, R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, OH, C1-2 alkyl, C1-2 haloalkyl, C1-2 alkoxy and C1-2 haloalkoxy. In some embodiments, R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, OH, and C1-2 alkyl; preferably hydrogen, halogen and OR13; more preferably hydrogen, fluoro and OH. In some embodiments, R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen and OH. In some embodiments, only one of R4, R5, R6and R8is other than hydrogen. In some embodiments, R4is other than hydrogen. In some embodiments, R5is other than hydrogen. In some embodiments, R6is other than hydrogen. In some embodiments, R8is other than hydrogen. In some embodiments, R4is hydrogen. In some embodiments, R5is hydrogen. In some embodiments, R6is hydrogen. In some embodiments, R7is hydrogen. In some embodiments, R8is hydrogen. In some embodiments, R9is hydrogen. In some embodiments, R10is hydrogen. In some embodiments, R4is not OR13. In some embodiments, R4is not OC1- 6alkyl. In some embodiments, R4is not OMe. In some embodiments, R5is not OR13. In some embodiments, R5is not OC1- 6alkyl. In some embodiments, R5is not OMe. In some embodiments, R6is not OR13. In some embodiments, R6is not OC1- 6alkyl. In some embodiments, R6is not OMe. In some embodiments, R8is not OR13. In some embodiments, R8is not OC1- 6alkyl. In some embodiments, R8is not OMe. In some embodiments, R7, R9and R10are each H. In some embodiments, R9and R10are each H. In some embodiments, R7and R10are each H. In some embodiments, R7is H. In some embodiments, R9is H. In some embodiments, R10is H. R11to R13In some embodiments, each R11is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl and C2-6haloalkynyl. In some embodiments, each R11is independently selected from hydrogen and C1-6alkyl. In some embodiments, each R12is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl and C1-6haloalkyl. In some embodiments, each R12is independently selected from hydrogen and C1-6alkyl. In some embodiments, each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl and C1-6haloalkyl. In some embodiments, each R13is independently selected from hydrogen and C1-6alkyl, preferably hydrogen and C1-3 alkyl, more preferably hydrogen and C1alkyl. In some embodiments, each R13is hydrogen. In some embodiments, each R13is C1-6alkyl, preferably C1-3 alkyl, more preferably C1alkyl. Additional embodiments In some embodiments, the compound of formula (I) is provided as a compound of formula (II): wherein R1, R2, R3, R4and L are as defined herein. In embodiments, L is methylene and R3is H. In embodiments, R4is selected from OH, OCH3and F. In some embodiments, R1and R2together with the nitrogen to which they are attached form any one of the following: . In some embodiments, the compound of formula (I) is provided as a compound of formula (III):

[0010] wherein R1, R2, R3, R5and L are as defined herein. In embodiments, L is methylene and R3is H. In embodiments, R5is selected from OH, OCH3and F. In some embodiments, R1and R2together with the nitrogen to which they are attached form any one of the following: . In some embodiments, the compound of formula (I) is provided as a compound of formula (IV): wherein R1, R2, R3, R6and L are as defined herein. In embodiments, L is methylene and R3is H. In embodiments, R6is selected from OH, OCH3and F. In embodiments, R6is selected from OH and F. In embodiments, R6is -OH. In embodiments, R6is -OCH3. In emodiments, R6is halo. In embodiments, R6is F. In some embodiments, R1and R2together with the nitrogen to which they are attached form any one of the following: In some embodiments of the compound of formula (IV), one of R1and R2is H and the other is as defined herein. In some embodiments, R1is CH3. In some embodiments, R2is CH3. In some embodiments, each of R1and R2is CH3. In some embodiments, the compound of formula (I) is provided as a compound of formula (V):

[0011] wherein R1, R2, R3, R8and L are as defined herein. In embodiments, L is methylene and R3is H. In embodiments, R8is selected from OH, OCH3and F. In embodiments, R8is selected from OH and halo. In embodiments, R8is selected from OH and F. In some embodiments, R1and R2together with the nitrogen to which they are attached form any one of the following: . In some embodiments of the compound of formula (V), one of R1and R2is H and the other is as defined herein. In some embodiments, R1is CH3. In some embodiments, R2is CH3. In some embodiments, each of R1and R2is CH3. In some embodiments, the compound of formula (I) is provided as a compound of formula (VI):

[0012] wherein R1, R2, R3, R4, R6, R8and L are as defined herein. In embodiments, L is methylene. In embodiments, R3is H. In embodiments, two of R4, R6and R8are H, and the other of R4, R6and R8is as defined herein with the proviso that it is not H. In embodiments, R6is selected from OH, OCH3and F. In these embodiments, R4and R8may each be H. In embodiments, R6is selected from OH and halo. In these embodiments, R4and R8may each be H. In embodiments, R6is selected from OH and F. In these embodiments, R4and R8may each be H. In embodiments, R4is selected from OH, OCH3and F. In these embodiments, R6and R8may each be H. In embodiments, R8is selected from OH, OCH3and F. In these embodiments, R4and R6may each be H. In some embodiments, R1and R2together with the nitrogen to which they are attached form any one of the following: . In some embodiments, one of R1and R2is H and the other is as defined herein. In some embodiments, each of R1and R2is H. Compounds In some embodiments, the compound of the invention is selected from the compounds of Table 1, or a pharmaceutically acceptable salt, solvate, tautomer, N- oxide, stereoisomer and / or prodrug thereof. Table 1: Compounds of the invention

[0013] In some embodiments, the compound of formula (I) is selected from any one of compounds I-1 to I-12, I-44 to I-50, and I-68-76, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer and / or prodrug thereof. In some embodiments, the compound of formula (I) is selected from any one of compounds I-44, I-68, I-69, and I-76, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer and / or prodrug thereof. Forms of the compound In the case of compounds that are solids, it will be understood by those skilled in the art that the inventive compounds, agents and salts may exist in different crystalline or polymorphic forms, all of which are intended to be within the scope of the present invention and specified formulae. The invention includes all crystalline forms of a compound of Formula (I) including anhydrous crystalline forms, hydrates, solvates and mixed solvates. If any of these crystalline forms demonstrates polymorphism, all polymorphs are within the scope of this invention. Formula (I) is intended to cover, where applicable, solvated as well as unsolvated forms of the compounds. Thus, Formula (I) includes compounds having the indicated structures, including the hydrated or solvated forms, as well as the non-hydrated and non-solvated forms. The compounds of Formula (I) or salts, tautomers, N-oxides, polymorphs or prodrugs thereof may be provided in the form of solvates. Solvates contain either stoichiometric or non-stoichiometric amounts of a solvent, and may be formed during the process of crystallization with pharmaceutically acceptable solvents such as water, alcohols such as methanol, ethanol or isopropyl alcohol, DMSO, acetonitrile, dimethyl formamide (DMF), acetic acid, and the like with the solvate forming part of the crystal lattice by either non-covalent binding or by occupying a hole in the crystal lattice. Hydrates are formed when the solvent is water, alcoholates are formed when the solvent is alcohol. Solvates of the compounds of the present invention can be conveniently prepared or formed during the processes described herein. In general, the solvated forms are considered equivalent to the unsolvated forms for the purposes of the invention. Basic nitrogen-containing groups may be quarternised with such agents as C1- 6alkyl halide, such as methyl, ethyl, propyl, and butyl chlorides, bromides and iodides; dialkyl sulfates like dimethyl and diethyl sulfate; and others. Nitrogen containing groups may also be oxidised to form an N-oxide. The compound of Formula (I) or salts, tautomers, N-oxides, solvates and / or prodrugs thereof that form crystalline solids may demonstrate polymorphism. All polymorphic forms of the compounds, salts, tautomers, N-oxides, solvates and / or prodrugs are within the scope of the invention. The compound of Formula (I) may demonstrate tautomerism. Tautomers are two interchangeable forms of a molecule that typically exist within an equilibrium. Any tautomers of the compounds of Formula (I) are to be understood as being within the scope of the invention. The compound of Formula (I) may contain one or more stereocentres. All stereoisomers of the compounds of formula (I) are within the scope of the invention. Stereoisomers include enantiomers, diastereomers, geometric isomers (E and Z olephinic forms and cis and trans substitution patterns) and atropisomers. In some embodiments, the compound is a stereoisomerically enriched form of the compound of formula (I) at any stereocentre. The compound may be enriched in one stereoisomer over another by at least about 60, 70, 80, 90, 95, 98 or 99%. The compound of Formula (I) or its salts, tautomers, solvates, N-oxides, and / or stereoisomers, may be isotopically enriched with one or more of the isotopes of the atoms present in the compound. For example, the compound may be enriched with one or more of the following minor isotopes:2H,3H,13C,14C,15N and / or17O, preferably2H. An isotope may be considered enriched when its abundance is greater than its natural abundance. A "prodrug" is a compound that may not fully satisfy the structural requirements of the compounds provided herein, but is modified in vivo, following administration to a subject or patient, to produce a compound of formula (I) provided herein. For example, a prodrug may be an acylated derivative of a compound as provided herein. Prodrugs include compounds wherein hydroxy, carboxy, amine or sulfhydryl groups are bonded to any group that, when administered to a mammalian subject, cleaves to form a free hydroxy, carboxy, amino, or sulfhydryl group, respectively. Examples of prodrugs include, but are not limited to, acetate, formate, phosphate and benzoate derivatives of alcohol and amine functional groups within the compounds provided herein. Prodrugs of the compounds provided herein may be prepared by modifying functional groups present in the compounds in such a way that the modifications are cleaved in vivo to generate the parent compounds. Prodrugs include compounds wherein an amino acid residue, or a polypeptide chain of two or more (eg, two, three or four) amino acid residues which are covalently joined to free amino, and amido groups of compounds of Formula (I). The amino acid residues include the 20 naturally occurring amino acids commonly designated by three letter symbols and also include, 4-hydroxyproline, hydroxylysine, demosine, isodemosine, 3-methylhistidine, norvlin, beta-alanine, gamma-aminobutyric acid, citrulline, homocysteine, homoserine, ornithine and methionine sulfone. Prodrugs also include compounds wherein carbonates, carbamates, amides and alkyl esters which are covalently bonded to the above substituents of Formula (I) through the carbonyl carbon prodrug sidechain. Compositions, formulations and modes of administration The compounds of formula (I) can be administered alone or in the form of a pharmaceutical composition. In practice, the compounds of formula (I) are usually administered in the form of pharmaceutical compositions, that is, in admixture with at least one pharmaceutically acceptable excipient. The proportion and nature of any pharmaceutically acceptable excipient(s) are determined by the properties of the selected compound of the invention, the chosen route of administration, and standard pharmaceutical practice. In another embodiment, there is provided a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, metabolite, or polymorph thereof, and at least one pharmaceutically acceptable excipient. Pharmaceutical compositions of the disclosure typically include a therapeutically effective amount of one or more active ingredients in admixture with one or more pharmaceutically and physiologically acceptable formulation materials. Suitable formulation materials include, but are not limited to, antioxidants, preservatives, coloring, flavoring and diluting agents, emulsifying agents, suspending agents, solvents, fillers, bulking agents, buffers, delivery vehicles, diluents, excipients and / or pharmaceutical adjuvants. For example, a suitable vehicle may be water for injection, physiological saline solution, or artificial perilymph, possibly supplemented with other materials common in compositions for parenteral administration. Neutral buffered saline or saline mixed with serum albumin are further exemplary vehicles. Pharmaceutical compositions of the present disclosure additionally comprise a pharmaceutically acceptable carrier, which, as used herein, includes any and all solvents, diluents, or other liquid vehicle, dispersion or suspension aids, surface active agents, isotonic agents, thickening or emulsifying agents, preservatives, solid binders, lubricants and the like, as suited to the particular dosage form desired. Remington's Pharmaceutical Sciences, Sixteenth Edition, E. W. Martin (Mack Publishing Co., Easton, Pa., 1980) discloses various carriers used in formulating pharmaceutical compositions and known techniques for the preparation thereof. Except insofar as any conventional carrier medium is incompatible with the compounds of the invention, such as by producing any undesirable biological effect or otherwise interacting in a deleterious manner with any other component(s) of the pharmaceutical composition, its use is contemplated to be within the scope of this disclosure. Some examples of materials which can serve as pharmaceutically acceptable carriers include, but are not limited to, sugars such as lactose, glucose and sucrose; starches such as corn starch and potato starch; cellulose and its derivatives such as sodium carboxymethyl cellulose, ethyl cellulose and cellulose acetate; powdered tragacanth; malt; gelatine; talc; excipients such as cocoa butter and suppository waxes; oils such as peanut oil, cottonseed oil; safflower oil, sesame oil; olive oil; corn oil and soybean oil; glycols; such as propylene glycol; esters such as ethyl oleate and ethyl laurate; agar; buffering agents such as magnesium hydroxide and aluminium hydroxide; alginic acid; pyrogenfree water; isotonic saline; Ringer's solution; ethyl alcohol, and phosphate buffer solutions, as well as other non-toxic compatible lubricants such as sodium lauryl sulfate and magnesium stearate, as well as colouring agents, releasing agents, coating agents, sweetening, flavouring and perfuming agents, preservatives and antioxidants can also be present in the composition, according to the judgment of the formulator. Various dosage units are each preferably provided as a discrete dosage tablet, capsules, lozenge, dragee, gum, or other type of solid formulation. Capsules may encapsulate a powder, liquid, or gel. The solid formulation may be swallowed, or may be of a suckable or chewable type (either frangible or gum-like). The present invention contemplates dosage unit retaining devices other than blister packs; for example, packages such as bottles, tubes, canisters, packets. The dosage units may further include conventional excipients well-known in pharmaceutical formulation practice, such as binding agents, gellants, fillers, tableting lubricants, disintegrants, surfactants, and colorants; and for suckable or chewable formulations. A compound of formula (I) may be administered in any form and route which makes the compound bioavailable. Compositions described herein may be administered systemically or directly to the site of condition or disease. Compositions described herein may be formulated from compounds according to Formula (I) for any appropriate route of administration including, for example, oral, rectal, nasal, vaginal, topical (including transdermal, buccal, ocular and sublingual), parenteral (including subcutaneous, intraperitoneal, intradermal, intravascular (for example, intravenous), intramuscular, spinal, intracranial, intrathecal, intraocular, periocular, intraorbital, intrasynovial and intraperitoneal injection, intracisternal injection as well as any other similar injection or infusion techniques), inhalation, insufflation, infusion or implantation techniques (e.g., as sterile injectable aqueous or non-aqueous solutions or suspensions). In some embodiments, compositions described herein may be administered orally, nasally, intravenously, intramuscularly, topically, subcutaneously, rectally, vaginally or by urethral application. Compositions intended for oral use may further comprise one or more components such as sweetening agents, flavouring agents, colouring agents and / or preserving agents in order to provide appealing and palatable preparations. Tablets contain the active ingredient in admixture with physiologically acceptable excipients that are suitable for the manufacture of tablets. Such excipients include, for example, inert diluents such as calcium carbonate, sodium carbonate, lactose, calcium phosphate or sodium phosphate, granulating and disintegrating agents such as corn starch or alginic acid, binding agents such as starch, gelatine or acacia, and lubricating agents such as magnesium stearate, stearic acid or talc. The tablets may be uncoated or they may be coated by known techniques to delay disintegration and absorption in the gastrointestinal tract and thereby provide a sustained action over a longer period. For example, a time delay material such as glyceryl monosterate or glyceryl distearate may be employed. Formulations for oral use may also be presented as hard gelatine capsules wherein the active ingredient is mixed with an inert solid diluent such as calcium carbonate, calcium phosphate or kaolin, or as soft gelatine capsules wherein the active ingredient is mixed with water or an oil medium such as peanut oil, liquid paraffin or olive oil. Oily suspensions may be formulated by suspending the active ingredients in a vegetable oil such as arachis oil, olive oil, sesame oil or coconut oil, or in a mineral oil such as liquid paraffin. The oily suspensions may contain a thickening agent such as beeswax, hard paraffin or cetyl alcohol. Sweetening agents such as those set forth above, and / or flavouring agents may be added to provide palatable oral preparations. Such suspensions may be preserved by the addition of an antioxidant such as ascorbic acid. Dispersible powders and granules suitable for preparation of an aqueous suspension by the addition of water provide the active ingredient in admixture with a dispersing or wetting agent, suspending agent and one or more preservatives. Suitable dispersing or wetting agents and suspending agents are exemplified by those already mentioned above. Additional excipients, such as sweetening, flavouring and colouring agents, may also be present. Pharmaceutical compositions may also be in the form of oil-in-water emulsions. The oily phase may be a vegetable oil such as olive oil or arachis oil, a mineral oil such as liquid paraffin, or a mixture thereof. Suitable emulsifying agents include naturally- occurring gums such as gum acacia or gum tragacanth, naturally-occurring phosphatides such as soy bean lecithin, and esters or partial esters derived from fatty acids and hexitol, anhydrides such as sorbitan monoleate, and condensation products of partial esters derived from fatty acids and hexitol with ethylene oxide such as polyoxyethylene sorbitan monoleate. An emulsion may also comprise one or more sweetening and / or flavouring agents. Syrups and elixirs may be formulated with sweetening agents, such as glycerol, propylene glycol, sorbitol or sucrose. Such Formulations may also comprise one or more demulcents, preservatives, flavouring agents and / or colouring agents. A composition may further include one or more components adapted to improve the stability or effectiveness of the applied formulation, such as stabilizing agents, suspending agents, emulsifying agents, viscosity adjusters, gelling agents, preservatives, antioxidants, skin penetration enhancers, moisturizers and sustained release materials. Examples of such components are described in Martindale – The Extra Pharmacopoeia (Pharmaceutical Press, London 1993) and Martin (ed.), Remington's Pharmaceutical Sciences. Formulations may comprise microcapsules, such as hydroxymethylcellulose or gelatine-microcapsules, liposomes, albumin microspheres, microemulsions, nanoparticles or nanocapsules. Preservatives include, but are not limited to, antimicrobials such as methylparaben, propylparaben, sorbic acid, benzoic acid, and formaldehyde, as well as physical stabilizers and antioxidants such as vitamin E, sodium ascorbate / ascorbic acid and propyl gallate. Suitable moisturizers include, but are not limited to, lactic acid and other hydroxy acids and their salts, glycerine, propylene glycol, and butylene glycol. Suitable emollients include lanolin alcohol, lanolin, lanolin derivatives, cholesterol, petrolatum, isostearyl neopentanoate and mineral oils. Suitable fragrances and colours include, but are not limited to, FD&C Red No.40 and FD&C Yellow No.5. Other suitable additional ingredients that may be included in a topical Formulation include, but are not limited to, abrasives, absorbents, anticaking agents, antifoaming agents, antistatic agents, astringents (such as witch hazel), alcohol and herbal extracts such as chamomile extract, binders / excipients, buffering agents, chelating agents, film forming agents, conditioning agents, propellants, opacifying agents, pH adjusters and protectants. Liquid dosage forms for oral administration include, but are not limited to, pharmaceutically acceptable emulsions, microemulsions, solutions, suspensions, syrups and elixirs. In addition to the active compounds, the liquid dosage forms may contain inert diluents commonly used in the art such as, for example, water or other solvents, solubilizing agents and emulsifiers such as ethyl alcohol, isopropyl alcohol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3- butylene glycol, dimethylformamide, oils (in particular, cottonseed, groundnut, corn, germ, olive, castor, and sesame oils), glycerol, tetrahydrofurfuryl alcohol, polyethylene glycols and fatty acid esters of sorbitan, and mixtures thereof. Besides inert diluents, the oral compositions can also include adjuvants such as wetting agents, emulsifying and suspending agents, sweetening, flavoring, and perfuming agents. Injectable preparations, for example, sterile injectable aqueous or oleaginous suspensions may be formulated according to the known art using suitable dispersing or wetting agents and suspending agents. The sterile injectable preparation may also be a sterile injectable solution, suspension or emulsion in a nontoxic parenterally acceptable diluent or solvent, for example, as a solution in 1,3-butanediol. Among the acceptable vehicles and solvents that may be employed are water, Ringer's solution, U.S. P. and isotonic sodium chloride solution. In addition, sterile, fixed oils are conventionally employed as a solvent or suspending medium. For this purpose any bland fixed oil can be employed including synthetic mono-or diglycerides. In addition, fatty acids such as oleic acid are used in the preparation of injectables. The injectable formulations can be sterilized, for example, by filtration through a bacterial-retaining filter, or by incorporating sterilizing agents in the form of sterile solid compositions which can be dissolved or dispersed in sterile water or other sterile injectable medium prior to use. A pharmaceutical composition may be formulated as inhaled formulations, including sprays, mists, or aerosols. For inhalation formulations, the composition or combination provided herein may be delivered via any inhalation methods known to a person skilled in the art. Such inhalation methods and devices include, but are not limited to, metered dose inhalers with propellants such as CFC or HFA or propellants that are physiologically and environmentally acceptable. Other suitable devices are breath operated inhalers, multidose dry powder inhalers and aerosol nebulizers. Aerosol formulations for use in the subject method typically include propellants, surfactants and co-solvents and may be filled into conventional aerosol containers that are closed by a suitable metering valve. Inhalant compositions may comprise liquid or powdered compositions containing the active ingredient that are suitable for nebulization and intrabronchial use, or aerosol compositions administered via an aerosol unit dispensing metered doses. Suitable liquid compositions comprise the active ingredient in an aqueous, pharmaceutically acceptable inhalant solvent such as isotonic saline or bacteriostatic water. The solutions are administered by means of a pump or squeeze-actuated nebulized spray dispenser, or by any other conventional means for causing or enabling the requisite dosage amount of the liquid composition to be inhaled into the patient's lungs. Suitable Formulations, wherein the carrier is a liquid, for administration, as for example, a nasal spray or as nasal drops, include aqueous or oily solutions of the active ingredient. Compositions suitable for rectal administration are preferably presented as unit dose suppositories. These may be prepared by at least partially dispersing the active in one or more lipophilic bases and then shaping the mixture. Pharmaceutical compositions may be formulated as sustained release formulations such as a capsule that creates a slow release of active following administration. Such formulations may generally be prepared using well-known technology and administered by, for example, oral, rectal or subcutaneous implantation, or by implantation at the desired target site. Carriers for use within such formulations are biocompatible, and may also be biodegradable. Preferably, the formulation provides a relatively constant level of active release. The amount of active contained within a sustained release formulation depends upon, for example, the site of implantation, the rate and expected duration of release and the nature of the condition to be treated. One skilled in the art can readily select the proper form and route of administration depending on the particular characteristics of the compound selected, the disease or condition to be treated, the stage of the disease or condition, and other relevant circumstances. It will be understood, that the specific dose level for any particular patient will depend upon a variety of factors including the activity of the specific compound employed, the age, body weight, general health, sex, diet, time of administration, route of administration, number of doses, and rate of excretion, drug combination (i.e. other drugs being used to treat the patient), and the severity of the particular disorder undergoing therapy. The phrase “therapeutically effective amount” generally refers to an amount of one or more active ingredients of the invention that (i) treats the particular disease, condition, or disorder, (ii) attenuates, ameliorates, or eliminates one or more sign or symptoms of the particular disease, condition, or disorder, or (iii) delays the onset of one or more sign or symptoms of the particular disease, condition, or disorder described herein. Typically, a therapeutically effective dosage is formulated to contain a concentration (by weight) of at least about 0.1% up to about 50% or more, and all combinations and sub-combinations of ranges therein. The compositions can be formulated to contain one or more actives described herein in a concentration of from about 0.1 to less than about 50%, for example, about 49, 48, 47, 46, 45, 44, 43, 42, 41 or 40%, with concentrations of from greater than about 0.1%, for example, about 0.2, 0.3, 0.4 or 0.5%, to less than about 40%, for example, about 39, 38, 37, 36, 35, 34, 33, 32, 31 or 30%. Exemplary compositions may contain from about 0.5% to less than about 30%, for example, about 29, 28, 27, 26, 25, 25, 24, 23, 22, 21 or 20%, with concentrations of from greater than about 0.5%, for example, about 0.6, 0.7, 0.8, 0.9 or 1%, to less than about 20%, for example, about 19, 18, 17, 16, 15, 14, 13, 12, 11 or 10%. The compositions can contain from greater than about 1% for example, about 2%, to less than about 10%, for example about 9 or 8%, including concentrations of greater than about 2%, for example, about 3 or 4%, to less than about 8%, for example, about 7 or 6%. The active agent can, for example, be present in a concentration of about 5%. In all cases, amounts may be adjusted to compensate for differences in amounts of active ingredients actually delivered to the treated cells or tissue. The frequency of administration may be once daily, 2, 3 or 4 times daily. The treatment period may be for the duration of the detectable disease. In some embodiments, the pharmaceutical composition comprises a compound according to any one of the herein disclosed embodiments, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, an additional therapeutic agent, and a pharmaceutically acceptable excipient. The additional agent may be any suitable agent described herein. In some embodiments, the additional agent is a psychoactive drug, including those described herein. In some embodiments, the additional agent is useful for treatment of a disease, disorder or condition by activation of a serotonin receptor, including those described herein. In some embodiments, the additional agent is selected from any one of the following, including those described herein: an agent for a mental illness and / or a neuropsychiatric condition; an agent for psychosis and / or psychotic symptoms; an agent for attention deficit hyperactivity disorder and / or attention deficit disorder; an agent for dementia and / or Alzheimer’s disease; and an agent for an addiction disorder. Applications The present disclosure provides methods of using the compounds of formula (I) and compositions as described herein. The present disclosure also provides methods of delivering to a subject in need thereof a compound of formula (I) or a composition (e.g., an effective amount of the compound or composition) of the present disclosure. In another aspect, the present disclosure provides methods of treating a disease in a subject in need thereof comprising administering to the subject in need thereof an effective amount (e.g., therapeutically effective amount) of a compound or composition (e.g., pharmaceutical composition) of the present disclosure. In another aspect, the present disclosure provides methods of preventing a disease in a subject in need thereof comprising administering to the subject in need thereof an effective amount (e.g., therapeutically effective amount) of a compound of formula (I) or composition (e.g., pharmaceutical composition) of the present disclosure. In another aspect, provided herein are uses of the compounds of formula (I) or compositions of the present disclosure in the manufacture of a medicament for use in a method (e.g., method of delivering an active agent to a subject in need thereof, method of treating a disease in a subject in need thereof, method of preventing a disease in a subject in need thereof) of the present disclosure. In another aspect, provided herein are uses of the compounds of formula (I) or compositions of the present disclosure in a method (e.g., method of delivering an active agent to a subject in need thereof, method of treating a disease in a subject in need thereof, method of preventing a disease in a subject in need thereof) of the present disclosure. In certain embodiments, the effective amount is effective in treating the disease. In certain embodiments, the effective amount is effective in preventing the disease. In another aspect, the present disclosure provides a method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. In another aspect, the present disclosure provides a method of preventing a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. In another aspect, the present disclosure provides method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein, in combination with another known agent useful for treatment of a disease, disorder or condition by activation of a serotonin receptor. The other known agents useful for treatment of a disease, disorder or condition by activation of a serotonin receptor may be any suitable agents known in the art, including those described herein. In another aspect, the present disclosure provides method of preventing a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein, in combination with another known agent useful for prevention of a disease, disorder or condition by activation of a serotonin receptor. In certain embodiments, the serotonin receptor is 5-HT2A. In certain embodiments, the serotonin receptor is one or both of 5-HT2A and 5- HT2C. Additionally, or alternatively, in some embodiments, the serotonin receptor is not 5-HT2B. In some embodiments, the compound of formula (I) of the present disclosure is selective towards the 5-HT2A receptor over one or both of the 5-HT2C receptor and the 5-HT2B receptor, preferably over the 5-HT2B receptor. In some embodiments, the compound of formula (I) is selective towards the 5-HT2C receptor over one or both of the 5-HT2A receptor and the 5-HT2B receptor, preferably over the 5-HT2B receptor. In some embodiments, the compound of formula (I) is selective toward the 5-HT2A receptor and 5-HT2C receptor over the 5-HT2B receptor. In some embodiments, the compound of formula (I) of the present disclosure exhibits an EC50 value for the 5-HT2A receptor of less than about 1 mM, less than about 100 µM, less than about 10 µM, less than about 1 µM, or less than about 100 nM, or less than about 10 nM, as determined by an assay described herein, for example an assay of calcium flux activity such as measuring changes in intracellular calcium. In some embodiments, the compound of formula (I) exhibits an EC50 for the 5-HT2A receptor of less than about 1 mM, less than about 900 µM, less than about 800 µM, less than about 700 µM, less than about 600 µM, less than about 500 µM, less than about 400 µM, less than about 300 µM, less than about 200 µM, less than about 100 µM, less than about 90 µM, less than about 80 µM, less than about 70 µM, less than about 60 µM, less than about 50 µM, less than about 40 µM, less than about 30 µM, less than about 20 µM, less than about 10 µM, less than about 9 µM, less than about 8 µM, less than about 7 µM, less than about 6 µM, less than about 5 µM, less than about 4 µM, less than about 3 µM, less than about 2 µM, less than about 1 µM, less than about 900 nM, less than about 800 nM, less than about 700 nM, less than about 600 nM, less than about 500 nM, less than about 400 nM, less than about 300 nM, less than about 200 nM, or less than about 100 nM, or any equivalent unit of measure (e.g., mol / L), as determined by an assay of calcium flux activity. In some embodiments, the compound of formula (I) of the present disclosure exhibits an EC50 value for the 5-HT2C receptor of less than about 1 mM, less than about 100 µM, less than about 10 µM, less than about 1 µM, or less than about 100 nM, or less than about 10 nM, as determined by an assay described herein, for example an assay of calcium flux activity such as measuring changes in intracellular calcium. In some embodiments, the compound of formula (I) exhibits an EC50 for the 5-HT2C receptor of less than about 1 mM, less than about 900 µM, less than about 800 µM, less than about 700 µM, less than about 600 µM, less than about 500 µM, less than about 400 µM, less than about 300 µM, less than about 200 µM, less than about 100 µM, less than about 90 µM, less than about 80 µM, less than about 70 µM, less than about 60 µM, less than about 50 µM, less than about 40 µM, less than about 30 µM, less than about 20 µM, less than about 10 µM, less than about 9 µM, less than about 8 µM, less than about 7 µM, less than about 6 µM, less than about 5 µM, less than about 4 µM, less than about 3 µM, less than about 2 µM, less than about 1 µM, less than about 900 nM, less than about 800 nM, less than about 700 nM, less than about 600 nM, less than about 500 nM, less than about 400 nM, less than about 300 nM, less than about 200 nM, or less than about 100 nM, or any equivalent unit of measure (e.g., mol / L), as determined by an assay of calcium flux activity. In some embodiments, the compound of formula (I) of the present disclosure exhibits an EC50 value for the 5-HT2B receptor of greater than about 1 µM, greater than about 10 µM, or greater than about 100 µM, as determined by an assay described herein, for example an assay of calcium flux activity such as measuring changes in intracellular calcium. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is a mental illness or a neuropsychiatric condition. Accordingly, the present application also includes a method of treating a mental illness or a neuropsychiatric condition comprising administering to a subject in need thereof a compound of formula (I) or a composition as described herein. The present application also includes a use of a compound of formula (I) of the present disclosure for treatment of a mental illness or a neuropsychiatric condition, as well as a use of a compound of formula (I) of the present disclosure for the preparation of a medicament for treatment of a mental illness or a neuropsychiatric condition. The application further includes a compound of formula (I) of the present disclosure for use in treating a mental illness or a neuropsychiatric condition. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is a mental illness or a neuropsychiatric condition and compound of formula (I) of the present disclosure is administered in combination with one or more additional agents for a mental illness or a neuropsychiatric condition. The one or more additional agents for a mental illness or a neuropsychiatric condition may be any suitable agents known in the art, including those described herein. In some embodiments, the additional agents for a mental illness or a neuropsychiatric condition is selected from antipsychotics, including typical antipsychotics and atypical antipsychotics; antidepressants including selective serotonin reuptake inhibitors (SSRIs) and selective norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants and monoamine oxidase inhibitors (MAOIs) (e.g. bupropion); anti-anxiety medication including benzodiazepines such as alprazolam; agents for an addiction disorder such as alcohol addiction (e.g., disulfiram), nicotine dependence (e.g., varenicline) and opioid use disorder (e.g., methadone, buprenorphine, buprenorphine-naloxone and buprenorphine long-acting injection); mood stabilizers such as lithium and anticonvulsants such carbamazepine, divalproex (valproic acid), lamotrigine, gabapentin and topiramate. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is neurodegeneration. Accordingly, the present application also includes a method of treating neurodegeneration comprising administering to a subject in need thereof a compound of formula (I) or a composition as described herein. The present application also includes a use of a compound of formula (I) of the present disclosure for treatment of neurodegeneration, as well as a use of a compound of formula (I) of the present disclosure for the preparation of a medicament for treatment neurodegeneration. The application further includes a compound of formula (I) of the present disclosure for use in treating neurodegeneration. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is reduced brain- derived neurotrophic factor (BDNF), mammalian target of rapamycin (mTOR) activation and / or inflammation. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor comprises cognitive impairment; ischemia including stroke; neurodegeneration; refractory substance use disorders; sleep disorders; pain, such as social pain, acute pain, cancer pain, chronic pain, breakthrough pain, bone pain, soft tissue pain, nerve pain, referred pain, phantom pain, neuropathic pain, cluster headaches and migraine; obesity and eating disorders; epilepsies and seizure disorders; neuronal cell death; excitotoxic cell death; or a combination thereof. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is psychosis or psychotic symptoms. Accordingly, the present application also includes a method of treating psychosis or psychotic symptoms comprising administering to a subject in need thereof a compound of formula (I) or a composition as described herein. The present application also includes a use of a compound of formula (I) of the present disclosure for treatment of psychosis or psychotic symptoms, as well as a use of a compound of formula (I) of the present disclosure for the preparation of a medicament for treatment of psychosis or psychotic symptoms. The application further includes a compound of formula (I) of the present disclosure for use in treating psychosis or psychotic symptoms. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is psychosis or psychotic symptoms and the the compound of formula (I) of the present disclosure is administered in combination with one or more additional agents for psychosis or psychotic symptoms. The one or more additional agents for psychosis or psychotic symptoms may be any suitable agents known in the art, including those described herein. In some embodiments, the additional agents for psychosis or psychotic symptoms are selected typical antipsychotics and atypical antipsychotics. The typical antipsychotics may be selected from acepromazine, acetophenazine, benperidol, bromperidol, butaperazine, carfenazine, chlorproethazine, chlorpromazine, chlorprothixene, clopenthixol, cyamemazine, dixyrazine, droperidol, fluanisone, flupentixol, fluphenazine, fluspirilene, haloperidol, levomepromazine, lenperone, loxapine, mesoridazine, metitepine, molindone, moperone, oxypertine, oxyprotepine, penfluridol, perazine, periciazine, perphenazine, pimozide, pipamperone, piperacetazine, pipotiazine, prochlorperazine, promazine, prothipendyl, spiperone, sulforidazine, thiopropazate, thioproperazine, thioridazine, thiothixene, timiperone, trifluoperazine, trifluperidol, triflupromazine and zuclopenthixol and combinations thereof. The atypical antipsychotics may be selected from amoxapine, amisulpride, aripiprazole, asenapine, blonanserin, brexpiprazole, cariprazine, carpipramine, clocapramine, clorotepine, clotiapine, clozapine, iloperidone, levosulpiride, lurasidone, melperone, mosapramine, nemonapride, olanzapine, paliperidone, perospirone, quetiapine, remoxipride, reserpine, risperidone, sertindole, sulpiride, sultopride, tiapride, veralipride, ziprasidone and zotepine, and combinations thereof. In some embodiments, administering to said subject in need thereof a therapeutically effective amount of the compound of formula (I) of the present disclosure does not result in a worsening of psychosis or psychotic symptoms such as, but not limited to, hallucinations and delusions. In some embodiments, administering to said subject in need thereof a therapeutically effective amount of the compound of formula (I) results in an improvement of psychosis or psychotic symptoms such as, but not limited to, hallucinations and delusions. In some embodiments, administering to said subject in need thereof a therapeutically effective amount of the compounds of formula (I) results in an improvement of psychosis or psychotic symptoms. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is a central nervous system (CNS) disease, disorder or condition and / or a neurological disease, disorder or condition. Accordingly, the present application also includes a method of treating a CNS disease, disorder or condition and / or a neurological disease, disorder or condition comprising administering a therapeutically effective amount of compound of formula (I) or a composition of the present disclosure to a subject in need thereof. The present application also includes a use of compound of formula (I) of the present disclosure for treatment a CNS disease, disorder or condition and / or a neurological disease, disorder or condition, as well as a use of compound of formula (I) of the present disclosure for the preparation of a medicament for treatment of a CNS disease, disorder or condition and / or a neurological disease, disorder or condition. The application further includes a compound of formula (I) of the present disclosure of the application for use in treating a CNS disease, disorder or condition and / or a neurological disease, disorder or condition. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is a central nervous system (CNS) disease, disorder or condition and / or a neurological disease, disorder or condition and the compound of formula (I) of the present disclosure is administered in combination with one or more additional agents for a central nervous system (CNS) disease, disorder or condition and / or a neurological disease, disorder or condition. The one or more additional agents for a central nervous system (CNS) disease, disorder or condition and / or a neurological disease, disorder or condition may be any suitable agents known in the art, including those described herein. In some embodiments, the additional agents for a central nervous system (CNS) disease, disorder or condition and / or a neurological disease, disorder or condition are selected from lithium, olanzapine, quetiapine, risperidone, ariprazole, ziprasidone, clozapine, divalproex sodium, lamotrigine, valproic acid, carbamazepine, topiramate, levomilnacipran, duloxetine, venlafaxine, citalopram, fluvoxamine, escitalopram, fluoxetine, paroxetine, sertraline, clomipramine, amitriptyline, desipramine, imipramine, nortriptyline, phenelzine, tranylcypromine, diazepam, alprazolam, clonazepam, or any combination thereof. Non limiting examples of standard of care therapy for depression are sertraline, fluoxetine, escitalopram, venlafaxine, or aripiprazole. Non-limiting examples of standard of care therapy for depression are citralopram, escitalopram, fluoxetine, paroxetine, diazepam, or sertraline. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is selected from attention deficit hyperactivity disorder and attention deficit disorder and a combination thereof. Accordingly, the present application also includes a method of treating attention deficit hyperactivity disorder and / or attention deficit disorder comprising administering to a subject in need thereof a compound of formula (I) or a composition as described herein. The present application also includes a use of a compound of formula (I) of the present disclosure for treatment of attention deficit hyperactivity disorder and / or attention deficit disorder, as well as a use of a compound of formula (I) of the present disclosure for the preparation of a medicament for treatment of attention deficit hyperactivity disorder and / or attention deficit disorder. The application further includes a compound of formula (I) of the present disclosure for use in treating attention deficit hyperactivity disorder and / or attention deficit disorder. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is attention deficit hyperactivity disorder and / or attention deficit disorder and a combination thereof and the compound of formula (I) of the present disclosure is administered in combination with one or more additional agents for attention deficit hyperactivity disorder and / or attention deficit disorder and a combination thereof. The one or more additional agents for attention deficit hyperactivity disorder and / or attention deficit disorder may be any suitable agents known in the art, including those described herein. In some embodiments, the additional agents for attention deficit hyperactivity disorder and / or attention deficit disorder and a combination thereof are selected from methylphenidate, dexamphetamine, lisdexamfetine, atomoxetine and amphetamine and a combination thereof. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is selected from dementia and Alzheimer’s disease and a combination thereof. Accordingly, the present application also includes a method of treating dementia and / or Alzheimer’s disease comprising administering to a subject in need thereof a compound of formula (I) or a composition as described herein. The present application also includes a use of a compound of formula (I) of the present disclosure for treatment of dementia and / or Alzheimer’s disease, as well as a use of a compound of formula (I) of the present disclosure for the preparation of a medicament for treatment of dementia and / or Alzheimer’s disease. The application further includes a compound of formula (I) of the present disclosure for use in treating dementia and / or Alzheimer’s disease. In some embodiments, the disease, disorder or condition that is treated by activation of a serotonin receptor is dementia or Alzheimer’s disease and the compound of formula (I) of the present disclosure is administered in combination with one or more additional agents for dementia or Alzheimer’s disease. The one or more additional agents for dementia or Alzheimer’s disease may be any suitable agents known in the art, including those described herein. In some embodiments, the additional agents for dementia and Alzheimer’s disease are selected from acetylcholinesterase inhibitors, NMDA antagonists and nicotinic agonists. The acetylcholinesterase inhibitors may be selected from donepezil, galantamine, rivastigmine, and phenserine, and combinations thereof. The NMDA antagonists may be selected from MK-801, ketamine, phencyclidine, and memantine, and combinations thereof. The nicotinic agonists may be selected from nicotine, nicotinic acid, nicotinic alpha7 agonists, or alpha2 beta4 agonists or a combination thereof. In another aspect, the present disclosure provides a method of treating a mental illness, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. In another aspect, the present disclosure provides a method of preventing a mental illness, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. The mental illness may be a neuropsychiatric condition. In certain embodiments, the mental illness is selected from anxiety disorders such as generalized anxiety disorder, panic disorder, social anxiety disorder and specific phobias; depression such as, hopelessness, loss of pleasure, fatigue and suicidal thoughts; mood disorders, such as depression, bipolar disorder, cancer-related depression, anxiety and cyclothymic disorder; psychotic disorders, such as hallucinations, delusions, mania, schizophrenia, schizoaffective disorder, schizophreniform Disorder; impulse control and addiction disorders, such as pyromania (starting fires), kleptomania (stealing) and compulsive gambling; alcohol addiction; drug addiction, such as opioid addiction / dependence, nicotine dependence, cocaine dependence, marijuana abuse and so on; smoking cessation; personality disorders, such as antisocial personality disorder, aggression, obsessive-compulsive personality disorder and paranoid personality disorder; obsessive-compulsive disorder (OCD), such as thoughts or fears that cause a subject to perform certain rituals or routines; post- traumatic stress disorder (PTSD); stress response syndromes (formerly called adjustment disorders); dissociative disorders, formerly called multiple personality disorder, or "split personality," and depersonalization disorder; factitious disorders; sexual and gender disorders, such as sexual dysfunction, gender identity disorder and the paraphilias; somatic symptom disorders, formerly known as a psychosomatic disorder or somatoform disorder. In certain embodiments, the mental illness is selected from hallucinations and delusions and a combination thereof. In these embodiments, the hallucinations may be selected from visual hallucinations, auditory hallucinations, olfactory hallucinations, gustatory hallucinations, tactile hallucinations, proprioceptive hallucinations, equilibrioceptive hallucinations, nociceptive hallucinations, thermoceptive hallucinations and chronoceptive hallucinations, and a combination thereof. In another aspect, the present disclosure provides a method for treating a central nervous system (CNS) disease, disorder or condition and / or a neurological disease, disorder or condition, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. In another aspect, the present disclosure provides a method for preventing a central nervous system (CNS) disease, disorder or condition and / or a neurological disease, disorder or condition, the method comprising administering to a subject in need thereof a compound of formula (I) or a pharmaceutical composition as described herein. In some embodiments, the CNS disease, disorder or condition and / or neurological disease, disorder or condition is selected from neurological diseases including neurodevelopmental diseases and neurodegenerative diseases such as Alzheimer’s disease; presenile dementia; senile dementia; vascular dementia; Lewy body dementia; cognitive impairment, Parkinson’s disease and Parkinsonian related disorders such as Parkinson dementia, corticobasal degeneration, and supranuclear palsy; epilepsy; CNS trauma; CNS infections; CNS inflammation; stroke; multiple sclerosis; Huntington’s disease; mitochondrial disorders; Fragile X syndrome; Angelman syndrome; hereditary ataxias; neuro-otological and eye movement disorders; neurodegenerative diseases of the retina amyotrophic lateral sclerosis; tardive dyskinesias; hyperkinetic disorders; attention deficit hyperactivity disorder and attention deficit disorders; restless leg syndrome; Tourette's syndrome; Tic disorder; schizophrenia; autism spectrum disorders; tuberous sclerosis; Rett syndrome; cerebral palsy; disorders of the reward system including eating disorders such as anorexia nervosa and bulimia nervosa; binge eating disorder, trichotillomania, dermotillomania, nail biting; migraine; fibromyalgia; and peripheral neuropathy of any etiology, and combinations thereof. In another aspect, the present disclosure provides a method for increasing neuronal plasticity, the method comprising contacting a neuronal cell with a compound of formula (I) or a pharmaceutical composition as described herein, in an amount sufficient to increase neuronal plasticity of the neuronal cell. “Neuronal plasticity” refers to the ability of the brain to change its structure and / or function continuously throughout a subject’s life. Examples of the changes to the brain include, but are not limited to, the ability to adapt or respond to internal and / or external stimuli, such as due to an injury, and the ability to produce new neurites, dendritic spines, and synapses. Increasing neuronal plasticity includes, but is not limited to, promoting neuronal growth, promoting neuritogenesis, promoting synaptogenesis, promoting dendritogenesis, increasing dendritic arbor complexity, increasing dendritic spine density, and increasing excitatory synapsis in the brain. In some embodiments, increasing neuronal plasticity comprises promoting neuronal growth, promoting neuritogenesis, promoting synaptogenesis, promoting dendritogenesis, increasing dendritic arbor complexity, and increasing dendritic spine density. In some embodiments, increasing neuronal plasticity can treat neurodegenerative disorder, Alzheimer’s, Parkinson’s disease, psychological disorder, depression, addiction, anxiety, post-traumatic stress disorder, treatment resistant depression, suicidal ideation, major depressive disorder, bipolar disorder, schizophrenia, stroke, traumatic brain injury, or substance use disorder. In another aspect the present disclosure provides methods of treating weight, comprising administering an effective amount of a compound of the invention to a subject in need thereof. Treatment of weight may include treating weight gain; weight loss; metabolic disorder; weight gain associated with pharmaceutical intervention; weight gain associated with a mental illness (including those described herein); eating disorders such as anorexia, bulimia, cachexia, etc.; eating behaviour; obesity; diabetes; insulin resistance; pre-diabetes; glucose intolerance; hyperlipidemia; and cardiovascular disease. In another aspect, the present disclosure provides a method for increasing dendritic spine density, the method comprising contacting a neuronal cell with a compound of formula (I) or a pharmaceutical composition as described herein, in an amount sufficient to increase dendritic spine density of the neuronal cell. In certain embodiments, the compound of formula (I) produces a maximum number of dendritic crossings with an increase of greater than 1.0 fold by a Sholl Analysis. In another aspect the present disclosure provides a method for activating a serotonin receptor in a cell, either in a biological sample or in a patient, comprising administering a compound of formula (I) as defined in any one of the herein disclosed embodiments to the cell. The serotonin receptor may be a 5-HT receptor subtype, preferably one or both of 5-HT2A and 5-HT2C. In some embodiments, effective amounts vary according to factors such as the disease state, age, sex and / or weight of the subject or species. In some embodiments, the amount of a given compound or compounds that will correspond to an effective amount will vary depending upon factors, such as the given drug(s) or compound(s), the pharmaceutical formulation, the route of administration, the type of condition, disease or disorder, the identity of the subject being treated and the like, but can nevertheless be routinely determined by one skilled in the art. In some embodiments, the compounds of formula (I) of the present disclosure are administered one, two, three or four times a year. In some embodiments, the compounds of the present disclosure are administered at least once a week. However, in another embodiment, the compounds are administered to the subject from about one time per two weeks, three weeks or one month. In another embodiment, the compounds are administered about one time per week to about once daily. In another embodiment, the compounds are administered 1, 2, 3, 4, 5 or 6 times daily. The length of the treatment period depends on a variety of factors, such as the severity of the disease, disorder or condition, the age of the subject, the concentration and / or the activity of the compounds of the application and / or a combination thereof. It will also be appreciated that the effective dosage of the compound used for the treatment may increase or decrease over the course of a particular treatment regime. Changes in dosage may result and become apparent by standard diagnostic assays known in the art. In some instances, chronic administration is required. For example, the compounds are administered to the subject in an amount and for duration sufficient to treat the subject. In some embodiments, the compounds of the application are administered at doses that are hallucinogenic or psychotomimetic and taken in conjunction with psychotherapy or therapy and may occur once, twice, three, or four times a year. However, in some embodiments, the compounds are administered to the subject once daily, once every two days, once every 3 days, once a week, once every two weeks, once a month, once every two months, or once every three months at doses that are not hallucinogenic or psychotomimetic. A compound of formula (I) of the present disclosure may be either used alone or in combination with other known agents useful for treating diseases, disorders or conditions by activation of a serotonin receptor, such as the compounds of the present disclosure. When used in combination with other known agents useful in treating diseases, disorders by activation of a serotonin receptor, it is an embodiment that a compound of formula (I) is administered contemporaneously with those agents. As used herein, "contemporaneous administration" of two substances to a subject means providing each of the two substances so that they are both active in the individual at the same time. The exact details of the administration will depend on the pharmacokinetics of the two substances in the presence of each other and can include administering the two substances within a few hours of each other, or even administering one substance within 24 hours of administration of the other, if the pharmacokinetics are suitable. Design of suitable dosing regimens is routine for one skilled in the art. In particular embodiments, two substances will be administered substantially simultaneously, i.e., within minutes of each other, or in a single composition that contains both substances. It is a further embodiment of the present application that a combination of agents is administered to a subject in a non-contemporaneous fashion. In some embodiments, a compound of formula (I) of the present disclosure is administered with another therapeutic agent simultaneously or sequentially in separate unit dosage forms or together in a single unit dosage form. Accordingly, the present application provides a single unit dosage form comprising one or more compounds of formula (I) as described herein, an additional therapeutic agent and a pharmaceutically acceptable carrier. In some embodiments, the compounds of the application are used or administered in an effective amount which comprises administration of doses or dosage regimens that are devoid of clinically meaningful psychedelic / psychotomimetic actions. In some embodiments, the compounds of the application are used or administered in an effective amount which comprises administration of doses or dosage regimens that provide clinical effects similar to those exhibited by a human plasma psilocin Cmax of 4 ng / mL or less and / or human 5-HT2A human CNS receptor occupancy of 40% or less or those exhibited by a human plasma psilocin Cmax of 1 ng / mL or less and / or human 5- HT2A human CNS receptor occupancy of 30% or less. In some embodiments, the compounds of the application are used or administered in an effective amount which comprises administration of doses or dosage regimens that provide clinical effects similar to those exhibited by a human plasma psilocin Tmax in excess of 60 minutes, in excess of 120 minutes or in excess of 180 minutes. Kit In another embodiment there is provided a kit or article of manufacture including one or more compounds, pharmaceutically acceptable salt, stereoisomer, solvate, metabolite, or polymorph, and / or pharmaceutical compositions as described above. In other embodiments there is provided a kit for use in a therapeutic application mentioned above, the kit including: a container holding one or more compounds, pharmaceutically acceptable salt, stereoisomer, solvate, metabolite, or polymorph and / or pharmaceutical compositions as described herein; a label or package insert with instructions for use. It will be understood that the invention disclosed and defined in this specification extends to all alternative combinations of two or more of the individual features mentioned or evident from the text or drawings. All of these different combinations constitute various alternative aspects of the invention. Examples Reference will now be made to specific embodiments of the invention. While the synthetic protocols outlined below will describe specific embodiments of the invention, it is understood that the intention is not to limit the invention to those embodiments. On the contrary, the invention is intended to cover all alternatives, modifications, and equivalents, which may be included within the scope of the present invention and defined by the claims. One skilled in the art will recognise numerous methods and materials similar or equivalent to those described herein. The present invention is in no way limited to the materials and methods described. It will be understood that the choice of structural features or substitution patterns surrounding the core scaffolds outlined above will influence the selection of one process over another. Starting materials are available from commercial sources or may be readily prepared from available precursors following straightforward transformations that are well known to one skilled in the art. General In the examples below, unless otherwise stated, temperatures are given in degrees Celsius (°C); operations were carried out at room or ambient temperature, “rt,” or “RT,” (typically a range of from about 18-25 °C; evaporation of solvent was carried out using a rotary evaporator under reduced pressure (typically, 4.5-30 mm Hg) with a bath temperature of up to 60 °C; the course of reactions was typically followed by thin layer chromatography (TLC); melting points are uncorrected; products exhibited satisfactory1H NMR and / or microanalytical data; and the following conventional abbreviations are also used: L (litres), mL (millilitres), mmol (millimoles), g (grams), mg (milligrams), min (minutes), and h (hours). Unless otherwise specified, all solvents and reagents were purchased from suppliers and used without further purification. Reactions were conducted under a blanket of nitrogen unless otherwise stated. Compounds were visualized under UV lamp (254 nm).1H NMR spectra were recorded on a 300 MHz, 400 MHz, or 600 MHz NMR instrument as indicated. Column and flash chromatography was performed using SiO2as the stationary phase and “MeOH-NH3” refers to a 9:1 solution of methanol to 15M ammonia aqueous. Synthesis of compounds General Procedures In the examples below, unless otherwise stated, temperatures are given in degrees Celsius (°C); operations were carried out at room or ambient temperature, “rt,” or “RT,” (typically a range of from about 18-25 °C; evaporation of solvent was carried out using a rotary evaporator under reduced pressure (typically, 4.5-30 mm Hg) with a bath temperature of up to 60 °C; the course of reactions was typically followed by thin layer chromatography (TLC); melting points are uncorrected; products exhibited satisfactory1H NMR and / or microanalytical data; and the following conventional abbreviations are also used: L (litres), mL (millilitres), mmol (millimoles), g (grams), mg (milligrams), min (minutes), and h (hours). Unless otherwise specified, all solvents and reagents were purchased from suppliers and used without further purification. Reactions were conducted under a blanket of nitrogen unless otherwise stated. Compounds were visualized under UV lamp (254 nm).1H NMR spectra were recorded on a 300 MHz, 400 MHz, or 600 MHz NMR instrument as indicated. Column and flash chromatography was performed using SiO2as the stationary phase and “MeOH-NH3” refers to a 9:1 solution of methanol to 15 M aqueous ammonia. LCMS was carried out using the following conditions: General Procedure A: Formulation of hydrochloride salts from amines Starting freebase amine is dissolved in a minimal amount of solvent (MeOH, i- PrOH or mixture thereof) and acidified to pH 1 by addition of concentrated HCl (32- 37%). Precipitation is initiated by addition of Et2O and the mixture is left to stand at 0 °C. The product is collected by vacuum filtration and washed with Et2O. General Procedure B: Formulation of fumaric acid and maleic acid salts from amines A solution of freebase amine in a minimal amount of solvent (acetone or i-PrOH) is added to a hot solution of fumaric acid or maleic acid in either acetone or i-PrOH (1 – 3 eq., 0.02 – 0.2 M) and the mixture is heated to between 40 – 60 °C. The mixture is cooled and precipitation is initiated by addition of Et2O or hexane and then left to stand at 0 °C. The product is collected by vacuum filtration and washed with Et2O. Scheme 1: Compounds of general formula (I) can be synthesised from an appropriately substituted naphthaldehyde following the outlined sequence of steps in Scheme 1 or similar as one skilled in the art may utilise. In scheme 1, Rnrepresents any of substituents R4to R10as defined herein for formula (I). The skilled person will appreciate that Rnmay be a substituent on any of the positions corresponding to R4to R10and will be limited by the appropriate definition depending on where it is positioned around the naphthyl core. An appropriately substituted naphthaldehyde can be subjected to a Henry reaction to afford the corresponding nitroalkene which can be reduced to give compounds of general formula (I) wherein R1and R2are H. This primary amine can then be subjected to reductive N-alkylation with an appropriate aldehyde to give compounds of general formula (I) (exemplified by, but not limited to, Example I-2, I-4, I-68, I-76). In the case where Rnis a methoxy group, demethylation can be performed using boron tribromide to give the corresponding hydroxy compound (exemplified by, but not limited to, Example I-11, I-37, I-69). Scheme 1 Alternative Routes Utilised to Generate Exemplified Compounds: Scheme 2: Compounds of general formula (I) can be synthesized from an appropriately substituted naphthaldehyde following the outlined sequence of steps below or similar as one skilled in the art may utilise. As for scheme 1 above, in scheme 2, Rnrepresents any of substituents R4to R10as defined herein for formula (I). The skilled person will appreciate that Rnmay be a substituent on any of the positions corresponding to R4to R10and will be limited by the appropriate definition depending on where it is positioned around the naphthyl core. Naphthaldehydes can undergo a one carbon homologation through a Wittig reaction to generate methoxyvinylnaphthalenes that under hydrolytic conditions garner the appropriate aldehyde. Compounds of general formula (I) can be afforded via reductive amination with appropriately substituted amines (exemplified by, but not limited to, Example I-3, I-4, etc). In the case where Rnis a methoxy group, demethylation can be performed using boron tribromide to give the corresponding hydroxy compound (exemplified by, but not limited to, Example I-10, I- 11). Methods for Generating Required Naphthaldehydes: Scheme 3: In cases where the requisite naphthaldehyde is not commercially available, the starting naphthaldehydes can be accessed in numerous ways as one skilled in the art may be aware. Hydroxy and methoxy substituents are shown in scheme 3 as representative examples. Two of several exemplary methods utilised to synthesise exemplified compounds are provided. Appropriately halogenated hydroxynaphthalene starting reagents can be converted to the corresponding methyl ether before undergoing Bouveault aldehyde synthesis, involving metal-halogen exchange (lithiation or Grignard formation). The subsequent organometallic intermediate can be quenched with DMF and subsequently hydrolysed to access the required naphthaldehydes. Alternatively, hydroxy naphthoic acids can be simultaneously methylated and esterified followed by reduction to the primary alcohol which can be selectively oxidised to the aldehyde in numerous ways (Dess-Martin Periodinane, Pyridinium Chlorochromate etc).

[0014] Scheme 3 Scheme 4: Compounds of general formula (I) can be synthesised from an appropriately substituted tetralone following the outlined sequence of steps in Scheme 4 or similar as one skilled in the art may utilise. A 3,4-dihydronaphthalen-1(2H)-one with the appropriate aromatic substitution pattern can undergo a Wittig-Horner reaction to yield the intermediate 3,4-dihydronaphthalene ester which can be aromatised under oxidative conditions including using the oxidant 2,3-dichloro-5,6-dicyano-p- benzoquinone (DDQ) or by catalytic transfer hydrogenation to the corresponding 6,6- aromatic system. Ester hydrolysis under basic conditions allows access to a carboxylic acid intermediate which can undergo condensation reactions with a variety of amide coupling reagents and the appropriately substituted amine component. Subjecting the resulting amides to reductive conditions allows accessed to the desired compounds of general formula (I) (exemplified by Examples I-44 to I-46). Scheme 4 Alternatively, the ester can be subjected to reductive conditions, such as LiBH4 or LiAlH4, to afford the corresponding alcohol. The alcohol can be oxidised to the corresponding aldehyde for subsequent reductive alkylation or can be activated, such as by the formation of a methanesulfonate, to react with the appropriately substituted amine component, to access the desired compounds of general formula (I), as shown in Scheme 5, or similar as one skilled in the art may utilise. Scheme 5 Example 1: Synthesis of 2-(2-methoxynaphthalen-1-yl)ethan-1-amine (I-2) Step 1: 2-methoxy-1-naphthaldehyde (2) To a suspension of 2-hydroxy-1-naphthaldehyde (10 g, 58.1 mmol) and K2CO3 (16.1 g, 116 mmol) in DMF (20 mL) was added iodomethane (7.25 mL, 116 mmol) and the resulting suspension was stirred at 50 ºC for 16 h. The cooled reaction was diluted with 200 mL of water and extracted with EtOAc (100 mL x 3). The combined organic layer was washed with water (20 mL x 5), then brine (50 mL x 2) and then concentrated. The solid was triturated with hot hexane:Et2O (9:1, 50 mL) and the off-white solid was collected by vacuum filtration after cooling. The filtrate was concentrated and the process repeated to afford a second crop, for a combined weight of 10.3 g (95%).1H NMR (400 MHz, CDCl3) δ 10.89 (s, 1H), 9.28 (d, J = 8.7 Hz, 1H), 8.04 (d, J = 9.2 Hz, 1H), 7.76 (d, J = 8.1 Hz, 1H), 7.69 – 7.56 (m, 1H), 7.51 – 7.37 (m, 1H), 7.27 (d, J = 9.2 Hz, 1H), 4.03 (s, 3H).13C NMR (101 MHz, CDCl3) δ 192.1, 164.1, 137.7, 131.7, 123.0, 128.6, 128.4, 125.1, 124.9, 116.8, 112.7, 56.7. Step 2: (E)-2-methoxy-1-(2-nitrovinyl)naphthalene (3) A solution of 2-methoxy-1-naphthaldehyde (5 g, 26.9 mmol) and nitromethane (28.8 mL, 20 equiv., 537 mmol) was treated with NH4OAc (1.24 g, 16.1 mmol) and the resulting solution was stirred at 80 ºC for 3 h. The reaction was then diluted with abs. EtOH (50 mL) and H2O (10 mL) whilst still hot. The resulting suspension was allowed to cool to RT and the yellow solid was collected by vacuum filtration which was identified as the title compound (5.7 g, 93%). Step 3: 2-(2-methoxynaphthalen-1-yl)ethan-1-amine (4) An ice-cold solution of 2-methoxy-1-(2-nitroethenyl)naphthalene (5 g, 21.8 mmol) in anhydrous THF (100 mL) was treated portionwise with LiAlH4 (6.6 g, 174 mmol) at a rate that maintained a gentle effervescence. The reaction was then heated to reflux for 3 h and the cooled reaction was diluted with THF (200 mL) and then quenched with cold H2O (6 mL), 15% aq. NaOH (6 mL), and H2O (20 mL). The resulting suspension was stirred with anhydrous Na2SO4 for 30 min before being filtered through a celite plug. The plug was eluted with 1:1 EtOAc:MeOH until the filtrate no longer contained any product. The combined filtrate was concentrated in vacuo and the residue was purified by flash chromatography (SiO2, 1-8% MeOH-NH3in CH2Cl2) to afford the title compound as a brown oil (1.8 g, 41%) which was used in the next step without further purification. A sample (300 mg, 1.5 mmol) was formulated as the fumarate salt for characterisation which were colourless crystals (160 mg, 34%).1H NMR (400 MHz, DMSO-d6) δ 8.07 (d, J = 8.1 Hz, 1H), 7.94 – 7.82 (m, 2H), 7.55 – 7.48 (m, 1H), 7.45 (d, J = 9.1 Hz, 1H), 7.40 – 7.34 (m, 1H), 6.46 (s, 2H), 3.93 (s, 3H), 3.37 – 3.26 (m, 2H), 2.97 – 2.83 (m, 2H).13C NMR (101 MHz, DMSO-d6) δ 168.2, 154.6, 135.4, 132.4, 128.7, 128.7, 128.5, 126.8, 123.3, 122.6, 117.7, 113.6, 56.4, 38.4, 23.2;1H qNMR purity: 97.0% (ERETIC). Step 4: 2-(2-methoxynaphthalen-1-yl)-N,N-dimethylethan-1-amine fumarate (I- 2·fumarate) To a solution of 2-(2-methoxy-1-naphthyl)ethylamine (300 mg, 1.49 mmol) in (CH2Cl)2(10 mL) was added formaldehyde (37% w / w, 1.21 mL, 14.9 mmol) and NaBH(OAc)3 (1.5 g, 7.4 mmol) at RT and then stirred at RT for 16 h. The reaction was quenched with water (10 mL) and neutralised with saturated aq. Na2CO3. The mixture was diluted with CH2Cl2(20 mL) and the layers were separated. The aqueous layer was further extracted with CH2Cl2(50 mL x 3), and the combined organic layer was washed with water (10 mL x 3) and brine (20 mL x 2). The organic layer was dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by flash chromatography (SiO2, 0.1%-5% MeOH-NH3in CH2Cl2) to afford the title compound as a pale-yellow oil (260 mg) which was formulated as the fumarate salt according to general procedure B which was isolated as colourless crystals (288 mg, 63%). LCMS (Condition A): tR (4.798 min) m / z = 230.15 [M+H]+;1H NMR (400 MHz, DMSO-d6) δ 8.06 – 7.94 (m, 1H), 7.91 – 7.82 (m, 2H), 7.55 – 7.48 (m, 1H), 7.45 (d, J = 9.1 Hz, 1H), 7.40 – 7.30 (m, 1H), 6.57 (s, 3H), 3.93 (s, 3H), 3.38 – 3.26 (m, 2H), 2.93 – 2.82 (m, 2H), 2.67 (s, 6H).13C NMR (101 MHz, DMSO-d6) δ 167.2, 154.5, 134.7, 132.4, 128.8, 128.6, 128.6, 126.8, 123.4, 122.7, 118.0, 113.6, 56.5, 56.4, 42.7, 20.7.1H qNMR purity: 99.1% (ERETIC). Example 2: Synthesis of N-ethyl-2-(2-methoxynaphthalen-1-yl)-N-methylethan-1- amine (I-3) Step 1: 2-methoxy-1-(2-methoxyvinyl)naphthalene (6) To an ice-cold solution of 2-methoxy-1-naphthaldehyde (5.0 g, 26.8 mmol) in anhydrous THF (50 mL) was added potassium tert-butoxide (9.0 g, 80.4 mmol) followed by (methoxymethyl)triphenyl phosphonium chloride (18.4 g, 53.6 mmol) under an atmosphere of nitrogen gas. The resulting reaction mixture was stirred at 0 ºC for 1 h at which point the reaction mixture was poured into water (50 mL) and extracted with EtOAc (50 mL x 3). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by flash chromatography (0% to 50% EtOAc in hexane) to afford the title compound as a brown oil (4.5 g, 78%) which was a mixture of E and Z isomers which was used in the next step without further purification. Step 2: 2-(2-methoxynaphthalen-1-yl)acetaldehyde (7) To a stirred solution of 6-methoxy-1-(2-methoxyvinyl)naphthalene (4.5 g, 21.0 mmol) in THF (40 mL) was added 5 M aq. HCl (22.5 mL) at RT and the resulting reaction mixture was stirred at 50 ºC for 2 h. The reaction mixture was then quenched with saturated aq. NaHCO3(80 mL) and extracted with 10% MeOH in DCM (150 mL x 3). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford the title compound as a pale-yellow liquid (4.2 g, quant.).1H NMR (400 MHz, DMSO-d6): δ 9.69 (s, 1H), 7.80 – 7.96 (m, 3H), 7.43 – 7.52 (m, 2H), 7.31 – 7.40 (m, 1H), 4.18 (d, J = 1.2 Hz, 2H), 3.91 (s, 3H). Step 3: N-ethyl-2-(2-methoxynaphthalen-1-yl)-N-methylethan-1-amine (I-3) To a stirred solution of 2-(2-methoxynaphthalen-1-yl)acetaldehyde (900 mg, 4.5 mmol) in DCE (1 mL) was added N-methylethanamine (780 mg, 13.5 mmol) at RT under an atmosphere of nitrogen gas. The reaction was stirred for 30 min at this temperature, at which time the reaction mixture was cooled to 0 °C and treated portion wise with Na(OAc)3BH (1.7 g, 13.5 mmol). The reaction mixture was allowed to stir for 16 h at RT before being poured into saturated aq. NaHCO3(200 mL) and extracted with 10 % MeOH in DCM (200 mL x 3). The combined organic layer was dried over Na2SO4, filtered, and concentrated under reduced pressure. The crude mass obtained was purified by reverse phase column chromatography (product eluted at 10% MeCN in water) to afford the title compound (150 mg, 14%). LCMS (Condition B): tR (1.706 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.92 (d, J = 8.8 Hz, 1H), 7.81 – 7.87 (m, 2H), 7.49 - 7.53 (m, 1H), 7.42 (d, J = 8.8 Hz, 1H), 7.32 – 7.37 (m, 1H), 3.92 (s, 3H), 3.13 – 3.17 (m, 2H), 2.44 – 2.50 (m, 4H), 2.30 (s, 3H), 1.01 (t, J = 7.2 Hz, 3H). Step 4: N-ethyl-2-(2-methoxynaphthalen-1-yl)-N-methylethan-1-amine fumarate (I- 3·fumarate) N-ethyl-2-(2-methoxynaphthalen-1-yl)-N-methylethan-1-amine (70 mg, 0.29 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as a light-brown solid (70 mg, 67%). LCMS (Condition B): tR (1.275 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.97 (d, J = 8.4 Hz, 1H), 7.85 – 7.89 (m, 2H), 7.50 – 7.54 (m, 1H), 7.44 (d, J = 8.8 Hz, 1H), 7.34 – 7.39 (m, 1H), 6.56 (s, 2H), 3.94 (s, 3H), 3.22 – 3.27 (m, 2H), 2.67 – 2.77 (m, 4H), 2.48 – 2.55 (m, 3H), 1.10 (t, J = 6.8 Hz, 3H); HPLC purity: 95.2% (210 nm). Example 3: Synthesis of 1-(2-(ethyl(methyl)amino)ethyl)naphthalen-2-ol (I-10) Step 1: 1-(2-(ethyl(methyl)amino)ethyl)naphthalen-2-ol fumarate (I-10·fumarate) To a stirred solution of N-ethyl-2-(2-methoxynaphthalen-1-yl)-N-methylethan-1- amine (500 mg, 2.05 mmol) in CH2Cl2(5 mL) was added 1 M BBr3 in CH2Cl2(2.5 mL) at 0 °C under an atmosphere of nitrogen gas and the reaction was stirred at RT for 2 h. The reaction mixture was then poured into saturated aq. NaHCO3(20 mL) and extracted with 10% MeOH in CH2Cl2(30 mL x 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude material was purified by prep-HPLC to afford the title compound which was formulated as the fumarate salt according to general procedure B which was isolated as a light-brown solid (50 mg, 7%). LCMS (Condition B): tR (1.145 min) m / z = 230.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.92 (d, J = 8.4 Hz, 1H), 7.78 (d, J = 8.4 Hz, 1H), 7.67 (d, J = 8.4 Hz, 1H), 7.46 (t, J = 7.6 Hz, 1H), 7.28 (t, J = 7.6 Hz, 1H), 7.16 (d, J = 8.4 Hz, 1H), 6.56 (s, 2H), 3.23 (t, J = 7.6 Hz, 2H), 2.78 – 2.85 (m, 4H), 2.57 (s, 3H), 1.13 (t, J = 7.2 Hz, 3H); HPLC purity: 100% (210 nm). Example 4: Synthesis of N-(2-(2-methoxynaphthalen-1-yl)ethyl)propan-2-amine (I- 77) Step 1: N-(2-(2-methoxynaphthalen-1-yl)ethyl)propan-2-amine fumarate (I- 77·fumarate) To a solution of 2-(2-methoxy-1-naphthyl)ethylamine (200 mg, 1.0 mmol) in (CH2Cl)2(3 mL) was added acetone (0.15 mL, 2.0 mmol), followed by NaBH(OAc)3 (1.0 g, 4.97 mmol). The reaction was stirred at RT for 3 h and then quenched with water (10 mL), neutralised with saturated aq. Na2CO3, and then made more basic with 15% aq. NaOH (2 mL). The mixture was diluted with CH2Cl2(20 mL) and the layers were separated. The aqueous layer was further extracted with CHCl3:i-PrOH (20 mL x 3) and the combined organic layer was washed with brine (50 mL), then dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by flash chromatography (SiO2, 1-10% MeOH-NH3in CH2Cl2) to afford the title compound as a yellow oil which was formulated as the fumarate salt according to general procedure B which was isolated as colourless crystals (340 mg, 92%). LCMS (Condition A): tR (5.001 min) m / z = 244.20 [M+H]+;1H NMR (400 MHz, DMSO-d6) δ 8.09 (d, J = 8.6 Hz, 1H), 7.95 – 7.85 (m, 2H), 7.56 – 7.42 (m, 2H), 7.42 – 7.31 (m, 1H), 6.53 (s, 2H), 3.94 (s, 3H), 3.44 – 3.25 (m, 3H), 2.98 – 2.84 (m, 2H), 1.24 (d, J = 6.5 Hz, 6H).13C NMR (101 MHz, DMSO-d6) δ 167.88, 154.57, 135.15, 132.40, 128.73, 128.53, 128.48, 126.84, 123.34, 122.65, 117.58, 113.56, 56.42, 48.72, 43.15, 21.86, 18.88.1H qNMR purity: 98.2% (ERETIC). Example 5: Synthesis of N-(2-(2-methoxynaphthalen-1-yl)ethyl)-N-methylpropan- 2-amine (I-4) Step 1: N-(2-(2-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (I-4) To a solution of 2-(2-methoxy-1-naphthyl)ethylamine (1.0 g, 5.0 mmol) in ( CH2Cl)2(15 mL) was added acetone (0.74 mL, 9.94 mmol), followed by NaBH(OAc)3 (5.27 g, 24.8 mmol). The reaction was stirred at RT for 3 h, and then formaldehyde (37% w / w, 3.9 mL, 49.8 mmol) and NaBH(OAc)3 (2.1 g, 9.94 mmol) was added and the resulting solution was stirred at RT for 16 h. The reaction was quenched with water (50 mL) and neutralised with saturated aq. Na2CO3. The mixture was diluted with CH2Cl2(50 mL) and the layers were separated. The aqueous layer was further extracted with CH2Cl2(50 mL x 3) and the combined organic layer was washed with brine (50 mL), then dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by flash chromatography (SiO2, 0.1%-5% MeOH-NH3in CH2Cl2) to afford the title compound as a yellow oil (920 mg, 72%).1H NMR (400 MHz, DMSO-d6) δ 8.13 (d, J = 8.6 Hz, 1H), 8.10 – 7.99 (m, 2H), 7.76 – 7.65 (m, 1H), 7.62 (d, J = 9.0 Hz, 1H), 7.58 – 7.48 (m, 1H), 4.12 (s, 3H), 3.40 – 3.24 (m, 2H), 3.15 – 2.96 (m, 1H), 2.78 – 2.64 (m, 2H), 2.50 (s, 3H), 1.15 (d, J = 6.5 Hz, 6H).13C NMR (101 MHz, DMSO-d6) δ 154.3, 132.6, 128.8, 128.5, 127.7, 126.4, 123.1, 122.7, 120.9, 113.7, 56.5, 53.0, 52.8, 36.8, 23.4, 18.0. Step 2: N-(2-(2-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine fumarate (I- 4·fumarate) N-(2-(2-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (300 mg, 1.2 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as colourless crystals (287 mg, 66%). LCMS (Condition A): tR (5.071 min) m / z = 258.20 [M+H]+;1H NMR (400 MHz, DMSO-d6) δ 8.03 (d, J = 8.6 Hz, 1H), 7.90 – 7.83 (m, 2H), 7.55 – 7.41 (m, 2H), 7.36 (t, J = 7.4 Hz, 1H), 6.56 (s, 2H), 3.94 (s, 3H), 3.51 – 3.44 (m, 1H), 3.39 – 3.31 (m, 2H), 2.93 – 2.81 (m, 2H), 2.64 (s, 3H), 1.18 (d, J = 6.6 Hz, 6H).13C NMR (101 MHz, DMSO-d6) δ 167.5, 154.6, 134.9, 132.4, 128.8, 128.6, 128.6, 126.8, 123.3, 122.6, 118.1, 113.6, 56.5, 54.1, 51.6, 34.9, 20.8, 16.4.1H qNMR purity: 97.2% (ERETIC). Example 6: Synthesis of 1-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol (I-11) Step 1: 1-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol fumarate (I-11·fumarate) 1-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol (150 mg, 0.62 mmol) was synthesised following the same method as compound I-10, which was then formulated as the fumarate salt according to general procedure B which was isolated as an off- white solid (150 mg, 67%). LCMS (Condition B): tR (1.216 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, MeOD-d4): δ 7.95 (d, J = 8.0 Hz, 1H), 7.82 (d, J = 8.0 Hz, 1H), 7.74 (d, J = 9.2 Hz, 1H), 7.52 – 7.58 (m, 1H), 7.32 – 7.38 (m, 1H), 7.18 (d, J = 9.2 Hz, 1H), 6.78 (s, 2H), 3.80 – 3.88 (m, 1H), 3.49 – 3.56 (m, 2H), 3.40 – 3.48 (m, 1H), 3.20 – 3.28 (m, 1H), 2.98 (s, 3H), 1.42 (d, J = 6.4 Hz, 3H), 1.36 (d, J = 6.4 Hz, 3H); HPLC purity: 100% (210 nm). Example 7: Synthesis of 1-(2-(2-methoxynaphthalen-1-yl)ethyl)azetidine (I-6) Step 1: 1-(2-(2-methoxynaphthalen-1-yl)ethyl)azetidine fumarate (I-6·fumarate) 1-(2-(2-methoxynaphthalen-1-yl)ethyl)azetidine (70 mg, 0.29 mmol) was synthesised following the same method as compound I-3, which was then formulated as the fumarate salt according to general procedure B which was isolated as a light-brown solid (60 mg, 55%). LCMS (Condition B): tR (1.251 min) m / z = 242.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.97 (d, J = 8.8 Hz, 1H), 7.85 – 7.89 (m, 2H), 7.52 (t, J = 7.6 Hz, 1H), 7.44 (d, J = 9.2 Hz, 1H), 7.35 (t, J = 7.2 Hz, 1H), 6.56 (s, 2H), 3.94 (s, 3H), 3.65 (t, J = 7.6 Hz, 4H), 3.09 – 3.14 (m, 2H), 2.87 – 2.92 (m, 2H), 2.15 – 2.20 (m, 2H); HPLC purity: 100% (210 nm). Example 8: Synthesis of 1-(2-(azetidin-1-yl)ethyl)naphthalen-2-ol (I-13) Step 1: 1-(2-(azetidin-1-yl)ethyl)naphthalen-2-ol trifluoroacetate (I-13·trifluoroacetate) 1-(2-(azetidin-1-yl)ethyl)naphthalen-2-ol trifluoroacetate (80 mg, 0.23 mmol) was synthesised following the same method as compound I-10, with TFA used as a modifier in the mobile phase. LCMS (Condition B): tR (1.174 min) m / z = 228.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 10.02 (br. s, 1H), 9.78 (br. s, 1H), 7.91 (d, J = 8.8 Hz, 1H), 7.81 (d, J = 7.6 Hz, 1H), 7.72 (d, J = 8.8 Hz, 1H), 7.48 – 7.53 (m, 1H), 7.29 – 7.34 (m, 1H), 7.21 (d, J = 8.8 Hz, 1H), 4.12 – 4.21 (m, 2H), 4.00 – 4.10 (m, 2H), 3.28 – 3.35 (m, 2H), 3.14 – 3.19 (m, 2H), 2.38 - 2.49 (m, 1H), 2.26 – 2.34 (m, 1H); HPLC purity: 95.8% (210 nm). Example 9: Synthesis of 1-(2-(2-methoxynaphthalen-1-yl)ethyl)pyrrolidine (I-7) Step 1: 1-(2-(2-methoxynaphthalen-1-yl)ethyl)pyrrolidine fumarate (I-7·fumarate) 1-(2-(2-methoxynaphthalen-1-yl)ethyl)pyrrolidine (130 mg, 0.51 mmol) was synthesised following the same method as compound I-3, which was then formulated as the fumarate salt according to general procedure B which was isolated as a light-brown solid (110 mg, 50%). LCMS (Condition B): tR (1.306 min) m / z = 256.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.00 (d, J = 8.4 Hz, 1H), 7.85 – 7.89 (m, 2H), 7.51 – 7.54 (m, 1H), 7.45 (d, J = 9.2 Hz, 1H), 7.37 (t, J = 7.2 Hz, 1H), 6.57 (s, 2H), 3.94 (s, 3H), 3.30 – 3.35 (m, 2H), 3.01 – 3.08 (m, 4H), 2.91 – 2.98 (m, 2H), 1.82 – 1.89 (m, 4H); HPLC purity: 100% (210 nm). Example 10: Synthesis of 1-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol (I-14) Step 1: 1-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol fumarate (I-14·fumarate) 1-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol (190 mg, 0.79 mmol) was synthesised following the same method as compound I-10, which was then formulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (150 mg, 51%). LCMS (Condition B): tR (1.219 min) m / z = 242.2 [M+H]+;1H NMR (400 MHz, MeOD-d4): δ 7.94 (d, J = 8.8 Hz, 1H), 7.81 (d, J = 8.0 Hz, 1H), 7.73 (d, J = 8.8 Hz, 1H), 7.51 – 7.56 (m, 1H), 7.32 – 7.36 (m, 1H), 7.18 (d, J = 8.8 Hz, 1H), 6.78 (s, 2H), 3.78 – 3.86 (m, 2H), 3.51 – 3.56 (m, 2H), 3.42 – 3.48 (m, 2H), 3.18 – 3.23 (m, 2H), 2.13 – 2.24 (m, 2H), 2.05 – 2.09 (m, 2H); HPLC purity: 100% (210 nm). Example 11: Synthesis of N-ethyl-2-(2-fluoronaphthalen-1-yl)-N-methylethan-1- amine (I-61) Step 1: 2-fluoro-3,4-dihydronaphthalen-1(2H)-one (9) To a stirred solution of 3,4-dihydronaphthalen-1(2H)-one (10.0 g, 68.5 mmol) in MeOH (150 mL) was added Selectfluor (28.3 g, 82.0 mmol) and conc. aq. H2SO4 (0.3 mL) at RT. The reaction mixture was stirred at 50 ºC for 16 h and then the cooled reaction was poured into water (200 mL) and extracted with EtOAc (200 mL x 2). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduce pressure. The residue was purified by flash chromatography (SiO2, 0% to 4 % EtOAc in hexane) to afford the title compound as a yellow oil (6.0 g, 53%).1H NMR (400 MHz, CDCl3): δ 8.09 (d, J = 8.0 Hz, 1H), 7.55 (t, J = 7.6 Hz, 1H), 7.38 (t, J = 8.0 Hz, 1H), 7.28 - 7.30 (m, 1H), 5.09 - 5.25 (m, 1H), 3.14 - 3.17 (m, 2H), 2.57 - 2.64 (m, 1H), 2.36 - 2.43 (m, 1H). Step 2: Ethyl 2-(2-fluoro-3,4-dihydronaphthalen-1-yl)acetate (10) To a stirred solution of 2-fluoro-3,4-dihydronaphthalen-1(2H)-one (2.5 g, 15.24 mmol) in THF (7 mL) was added NaH (60% w / w in mineral oil, 0.8 g, 33.33 mmol) and ethyl 2-(diethoxyphosphoryl)acetate (2.5 g, 11.16 mmol) at 0 ºC. The resulting reaction mixture was stirred at 70 °C for 16 h. before being quenched with water (200 mL) and extracted with EtOAc (200 mL x 2). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduce pressure. The residue was purified by flash chromatography (SiO2, 0% to 1% EtOAc in hexane) to afford the title compound as a yellow oil (2.3 g, 65%).1H NMR (400 MHz, CDCl3): δ 7.22 - 7.28 (m, 1H), 7.11 - 7.14 (m, 3H), 4.17 (q, J = 7.2 Hz, 2H), 3.54 - 3.56 (m, 2H), 2.99 – 3.04 (m, 2H), 2.60 - 2.65 (m, 2H), 1.25 (t, J = 7.2 Hz, 3H). Step 3: Ethyl 2-(2-fluoronaphthalen-1-yl)acetate (11) To a stirred solution ethyl 2-(2-fluoro-3,4-dihydronaphthalen-1-yl)acetate (2.3 g, 9.83 mmol) in toluene (80.5 mL) was added DDQ (2.6 g, 11.79 mmol) at RT. The reaction mixture was stirred at 120 °C for 3 h before being filtered. The filtrate was diluted with EtOAc (200 mL) and washed with brine (100 mL) before being dried over anhydrous Na2SO4 and concentrated under reduce pressure. The residue was purified by flash chromatography (SiO2, 0% to 3% EtOAc in hexane) to afford the title compound as a brown oil (2.0 g, 88%).1H NMR (400 MHz, CDCl3): δ 7.93 (d, J = 8.4 Hz, 1H), 7.87 (d, J = 8.0 Hz, 1H), 7.79 - 7.83 (m, 1H), 7.58 (t, J = 7.2 Hz, 1H), 7.45 - 7.49 (m, 1H), 7.29 (d, J = 9.2 Hz, 1H), 4.18 (q, J = 7.2 Hz, 2H), 4.12 (d, J = 1.6 Hz, 2H), 1.25 (t, J = 7.2 Hz, 3H). Step 4: 2-(2-fluoronaphthalen-1-yl)ethan-1-ol (12) To an ice-cold stirred solution of ethyl 2-(2-fluoronaphthalen-1-yl)acetate (2.0 g, 8.62 mmol) in THF (20 mL) was added LiAlH4 (0.47 g, 12.92 mmol) in portions. The reaction mixture was then stirred at RT for 1 h before the reaction was quenched by slow addition into water (200 mL). The resulting mixture was extracted with EtOAc (200 mL x 3) and the combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford the title compound as a yellow oil (1.8 g) which was used in the next step without further purification.1H NMR (400 MHz, CDCl3): δ 8.07 (d, J = 8.0 Hz, 1H), 7.86 (d, J = 8.0 Hz, 1H), 7.74 - 7.78 (m, 1H), 7.58 (t, J = 7.2 Hz, 1H), 7.45 -7.49 (m, 1H), 7.25 - 7.31 (m, 1H), 3.98 (t, J = 6.8 Hz, 2H), 3.39 - 3.43 (m, 2H). Step 5: 2-(2-fluoronaphthalen-1-yl)ethyl methanesulfonate (13) To an ice-cold stirred solution of 2-(2-fluoronaphthalen-1-yl)ethan-1-ol (1.8 g, 9.47 mmol) in CH2Cl2(18 mL) was added TEA (2.8 g, 27.72 mmol) and MsCl (1.6 g, 14.4 mmol). The resulting reaction mixture was stirred at 0 ºC for 2 h before being quenched with water (100 mL) and extracted with EtOAc (100 mL x 2). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduce pressure to afford the title compound as a pale-yellow resin (1.4 g, 55%) which was used in the next step without further purification. Step 6: N-ethyl-2-(2-fluoronaphthalen-1-yl)-N-methylethan-1-amine (I-61) To a stirred solution 2-(2-fluoronaphthalen-1-yl)ethyl methanesulfonate (200 mg, 0.74 mmol) in MeCN (2 mL) was added N-methylethanamine (220 mg, 3.73 mmol) and K2CO3(510 g, 3.73 mmol) at RT. The resulting reaction mixture was stirred at 80 ºC for 16 h before being quenched with water (50 mL) and extracted with EtOAc (50 mL x 2). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduce pressure. The residue was purified by reverse phase column chromatography (product eluted at 56 % MeCN in H2O) to afford the title compound as a brown resin (75 mg, 44%). LCMS (Condition B): tR (1.255 min) m / z = 232.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.04 (d, J = 8.4 Hz, 1H), 7.96 (d, J = 8.4 Hz, 1H), 7.86 - 7.89 (m, 1H), 7.62 (t, J = 7.6 Hz, 1H), 7.48 - 7.52 (m, 1H), 7.37 - 7.42 (m, 1H), 3.18 - 3.22 (m, 2H), 2.51 - 2.57 (m, 2H), 2.42 - 2.50 (m, 2H), 2.86 (s, 3H), 0.97 (t, J = 6.8 Hz, 3H). Step 7: N-ethyl-2-(2-fluoronaphthalen-1-yl)-N-methylethan-1-amine fumarate (I- 61·fumarate) N-ethyl-2-(2-fluoronaphthalen-1-yl)-N-methylethan-1-amine (75 mg, 0.32 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as a white solid (95 mg, 86%). LCMS (Condition B): tR (1.680 min) m / z = 232.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.06 (d, J = 8.8 Hz, 1H), 7.96 (d, J = 8.4 Hz, 1H), 7.89 (dd, J = 8.8, 5.6 Hz, 1H), 7.62 (t, J = 7.6 Hz, 1H), 7.51 (t, J = 7.2 Hz, 1H), 7.41 (t, J = 9.2 Hz, 1H), 6.57 (s, 2H), 3.21 – 3.26 (m, 2H), 2.58 – 2.72 (m, 4H), 2.41 (s, 3H), 1.03 (t, J = 7.2 Hz, 3H); HPLC purity: 98.1% (210 nm). Example 12: Synthesis of N-(2-(2-fluoronaphthalen-1-yl)ethyl)-N-methylpropan-2- amine (I-62) Step 1: N-(2-(2-fluoronaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (I-62) To a stirred solution 2-(2-fluoronaphthalen-1-yl)ethyl methanesulfonate (450 mg, 1.67 mmol) in MeCN (5 mL) was added N-methylpropan-2-amine (610 mg, 8.38 mmol) and K2CO3 (1.15 g, 8.38 mmol) at RT. The reaction mixture was stirred at 80 °C for 16 h before being quenched with water (35 mL) and extracted with EtOAc (30 mL x 2). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduce pressure. The residue was purified by reverse phase column chromatography (product eluted at 59% MeCN in water) to afford the title compound as a yellow resin (90 mg, 22%). LCMS (Condition B): tR (1.285 min) m / z = 246.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.03 (d, J = 8.8 Hz, 1H), 7.95 (d, J = 8.0 Hz, 1H), 7.86 (dd, J = 8.8, 5.6 Hz, 1H), 7.61 (t, J = 7.6 Hz, 1H), 7.47 - 7.51 (m, 1H), 7.38 (t, J = 9.2 Hz, 1H), 3.12 - 3.16 (m, 2H), 2.77 - 2.84 (m, 1H), 2.55 - 2.57 (m, 2H), 2.38 (s, 3H), 0.84 - 0.92 (m, 6H). Step 2: N-(2-(2-fluoronaphthalen-1-yl)ethyl)-N-methylpropan-2-amine fumarate (I- 62·fumarate) N-(2-(2-fluoronaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (90 mg, 0.37 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as a light-brown solid (80 mg, 67%). LCMS (Condition B): tR (1.259 min) m / z = 246.2 [M+H]+;1H NMR (400 MHz, MeOD-d4): δ 8.12 (d, J = 8.4 Hz, 1H), 7.88 – 7.96 (m, 2H), 7.64 – 7.69 (m, 1H), 7.50 – 7.55 (m, 1H), 7.36 (t, J = 9.2 Hz, 1H), 6.74 (s, 1H), 3.71 – 3.75 (m, 1H), 3.53 – 3.59 (m, 2H), 3.25 – 3.29 (m, 2H), 2.91 (s, 3H), 1.35 (t, J = 6.8 Hz, 6H); HPLC purity: 98.3% (210 nm). Example 13: Synthesis of 1-(2-(2-fluoronaphthalen-1-yl)ethyl)azetidine (I-65) Step 1: 1-(2-(2-fluoronaphthalen-1-yl)ethyl)azetidine (I-65) To a stirred solution 2-(2-fluoronaphthalen-1-yl)ethyl methanesulfonate (200 mg, 0.75 mmol) in MeCN (5 mL) was added azetidine (210 mg, 3.72 mmol) and K2CO3 (510 mg, 3.72 mmol) at RT. The reaction mixture was stirred at 80 ºC for 16 h before being quenched with water (50 mL) and extracted with EtOAc (50 mL x 2). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduce pressure. The residue was purified by reverse phase column chromatography (product eluted at 58 % MeCN in water) to afford the title compound as a brown resin (130 mg, 76%). LCMS (Condition B): tR (1.228 min) m / z = 230.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.03 (d, J = 8.4 Hz, 1H), 7.95 (d, J = 8.4 Hz, 1H), 7.87 (dd J = 8.8, 5.6 Hz, 1H), 7.61 (t, J = 7.6 Hz, 1H), 7.48 - 7.52 (m, 1H), 7.39 (t, J = 9.2 Hz, 1H), 3.11 (t, J = 6.8 Hz, 4H), 2.98 – 3.03 (m, 2H), 2.57 (t, J = 7.6 Hz, 2H), 1.94 (p, J = 6.8 Hz, 2H). Step 2: 1-(2-(2-fluoronaphthalen-1-yl)ethyl)azetidine fumarate (I-65·fumarate) 1-(2-(2-fluoronaphthalen-1-yl)ethyl)azetidine (130 mg, 0.56 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (220 mg, quant.). LCMS (Condition B): tR (1.197 min) m / z = 230.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.06 (d, J = 8.4 Hz, 1H), 7.96 (d, J = 8.0 Hz, 1H), 7.90 (dd, J = 8.8, 5.6 Hz, 1H), 7.61 (t, J = 7.6 Hz, 1H), 7.51 (t, J = 7.6 Hz, 1H), 7.41 (t, J = 9.2 Hz, 1H), 6.56 (s, 2H), 3.43 (t, J = 7.2 Hz, 4H), 3.07 – 3.12 (m, 2H), 2.81 – 2.85 (m, 2H), 2.05 – 2.10 (m, 2H); HPLC purity: 99.5% (210 nm). Example 14: Synthesis of 1-(2-(2-fluoronaphthalen-1-yl)ethyl)pyrrolidine fumarate (I-66) Step 1: 1-(2-(2-fluoronaphthalen-1-yl)ethyl)pyrrolidine fumarate (I-66) To a stirred solution 2-(2-fluoronaphthalen-1-yl)ethyl methanesulfonate (450 mg, 1.68 mmol) in MeCN (10 mL) was added pyrrolidine (590 mg, 8.39 mmol) and K2CO3 (1.15 g, 8.39 mmol) at RT. The reaction mixture was stirred at 80 ºC for 16 h before being quenched with water (60 mL) and extracted with EtOAc (45 mL x 3). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduce pressure. The residue was purified by reverse phase column chromatography (product eluted at 72% MeCN in water) to afford the title compound as a yellow resin (200 mg, 44%). LCMS (Condition B): tR (1.306 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.04 (d, J = 8.4 Hz, 1H), 7.95 (d, J = 8.0 Hz, 1H), 7.87 (dd J = 8.8, 5.6 Hz, 1H), 7.61 (t, J = 7.6 Hz, 1H), 7.49 (t, J = 7.6 Hz, 1H), 7.39 (t, J = 9.2 Hz, 1H), 3.18 - 3.23 (m, 2H), 2.59 – 2.64 (m, 2H), 2.47 - 2.53 (m, 4H), 1.68 - 1.71 (m, 4H). Step 2: 1-(2-(2-fluoronaphthalen-1-yl)ethyl)pyrrolidine fumarate (I-66·fumarate) 1-(2-(2-fluoronaphthalen-1-yl)ethyl)pyrrolidine (80 mg, 0.32 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (95 mg, 81%). LCMS (Condition B): tR (1.700 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.09 (d, J = 8.4 Hz, 1H), 7.97 (d, J = 8.0 Hz, 1H), 7.90 (dd, J = 8.8, 5.6 Hz, 1H), 7.61 (t, J = 7.2 Hz, 1H), 7.51 (t, J = 7.6 Hz, 1H), 7.41 (t, J = 9.2 Hz, 1H), 6.55 (s, 2H), 3.27 – 3.33 (m, 2H), 2.85 - 2.89 (m, 6H), 1.73 – 1.86 (m, 4H); HPLC purity: 100% (210 nm). Example 15: Synthesis of N-ethyl-2-(3-methoxynaphthalen-1-yl)-N-methylethan-1- amine (I-17) Step 1: 1-bromo-3-methoxynaphthalene (15) To a stirred solution of 4-bromonaphthalen-2-ol (5.0 g, 22.42 mmol, 1.0 eq) in DMF (50 mL) was added NaH (3 g, 60% w / w dispersion in mineral oil, 40.3 mmol) in portions at 0 °C under an atmosphere of N2 gas. The reaction mass was stirred for 30 min at this temperature followed by the addition of MeI (12.7 g, 89.7 mmol). The resulting mixture was warmed to RT and stirred for an additional 3 h before being poured into H2O (1 L) and extracted with EtOAc (3 x 500 mL). The combined organics were dried over Na2SO4, filtered, and concentrated under reduced pressure to afford the title compound as a brown solid (5 g, 94% yield).1H NMR (400 MHz, CDCl3): δ 8.17-8.15 (m, 1H), 7.76-7.74 (m, 1H), 7.53-7.51 (m, 1H), 7.49-7.44 (m, 2H), 7.15 (d, J = 2.4 Hz, 1H), 3.94 (s, 3H). Step 2: 3-methoxy-1-naphthaldehyde (16) To a stirred solution of 1-bromo-3-methoxynaphthalene (5.0 g, 21.09 mmol) in dry THF (50 mL) at -78 °C was added dropwise a solution of n-BuLi (2.5M in THF, 25 mL, 42.19 mmol) over 15 minutes (80 mL) under an atmosphere of nitrogen gas and maintained at this temperature for a further 2 h. The reaction mass was then treated with DMF (2.5 mL, 52.74 mmol) dropwise. The reaction was warmed to RT and stirring continued for 4 h at which point the reaction mass was poured into saturated NH4Cl solution (500 mL) and extracted with EtOAc (3 x 500 mL). The combined organics were dried over Na2SO4 and concentrated under reduced pressure to give the title compound as a yellow oil.1H NMR (400 MHz, CDCl3): δ 10.39 (s, 1H), 7.10-7.85 (m, 2H), 7.77- 7.68 (m, 2H), 7.57-7.53 (m, 2H), 4.10 (s, 3H). Step 3: 3-methoxy-1-(2-methoxyvinyl) naphthalene (17) To a stirred solution of KOtBu (9.0 g, 80.6 mmol) in dry THF (50 mL) at 0 °C was added (methoxymethyl)triphenyl phosphonium chloride (22 g, 67.2 mmol) in portions over 30 min under an atmosphere of N2 gas, at which point the reaction was warmed to RT and stirring continued for an additional 30 min. The reaction mixture was then cooled to 0 °C and treated with 3-methoxy-1-naphthaldehyde (5.0 g, 26.88 mmol) in portions, warmed to RT and stirring continued for a further 3 h. The reaction was then poured into water (500 mL) and extracted with EtOAc (3 x 500 mL). The combined organics were dried over Na2SO4, before being filtered, concentrated under reduced pressure and the resultant crude material purified by flash column chromatography (2% EtOAc in hexanes) to give the title compound as a mixture of E / Z isomers as a pale yellow oil (4.5 g, 78%). E isomer: 1H NMR (400 MHz, CDCl3): δ 8.04 (t, J = 8.8 Hz, 1H), 7.78 (d, J = 8.0 Hz, 1H), 7.46-7.43 (m, 1H), 7.41-7.36 (m, 1H), 7.32-7.31 (m, 2H), 6.55- 6.46 (m, 1H), 3.87-3.85 (m, 3H). Step 4: 2-(3-methoxynaphthalen-1-yl) acetaldehyde (18) To a stirred solution of 3-methoxy-1-(2-methoxyvinyl)naphthalene (3.0 g, 14 mmol) in THF (30 mL) was added 2 M aq. HCl (15 mL) at RT and the resulting reaction mixture was stirred at 70 °C for 2 h. The reaction mixture was then quenched with saturated aq. NaHCO3(20 mL) and then extracted with EtOAc (150 mL x 3). The combined organic layers was dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure to afford the title compound as a yellow liquid (2.7 g, 96%).1H NMR (400 MHz, DMSO-d6): δ 9.74 (s, 1H), 7.85-7.79 (m, 3H), 7.47 (t, J = 7.6 Hz ,1H), 7.36 (t, J = 8.4 Hz ,1H), 7.28 (d, J = 2.4 Hz, 1H), 7.13 (d, J = 2.8 Hz, 1H), 4.21 (s, 2H), 3.87 (s, 3H). Step 5: N-ethyl-2-(3-methoxynaphthalen-1-yl)-N-methylethan-1-amine (I-17) To a stirred solution of 2-(3-methoxynaphthalen-1-yl)acetaldehyde (1.5 g, 7.5 mmol) in DCE (10 mL) was added N-methylethanamine (1.3 g, 22.5 mmol) at RT under an atmosphere of nitrogen gas. The reaction was stirred for 30 min at this temperature, at which time the reaction mixture was cooled to 0 °C and treated portion wise with Na(OAc)3BH (2.8 g, 22.5 mmol). The reaction mixture was allowed to stir for 16 h at RT before being poured into saturated aq. NaHCO3(500 mL) and extracted with 10 % MeOH in DCM (500 mL x 3). The combined organic layer was dried over Na2SO4, filtered, and concentrated under reduced pressure. The crude mass obtained was purified by reverse phase column chromatography (product eluted at 10% MeCN in water) to afford the title compound (940 mg, 52%). LCMS (Condition B): tR (1.633 min) m / z = 244.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.93 (d, J = 8.0 Hz, 1H), 7.79 (d, J = 8.0 Hz, 1H), 7.35 - 7.45 (m, 2H), 7.16 (s, 1H), 7.05 (s, 1H), 3.84 (s, 3H), 3.12 (t, J = 7.6 Hz, 2H), 2.61 (t, J = 7.6 Hz, 2H), 2.42 - 2.49 (m, 2H), 2.26 (s, 3H), 0.98 (t, J = 7.2 Hz, 3H); HPLC purity: 98.2% (210 nm). Step 6: N-ethyl-2-(3-methoxynaphthalen-1-yl)-N-methylethan-1-amine fumarate (I- 17·fumarate) N-ethyl-2-(3-methoxynaphthalen-1-yl)-N-methylethan-1-amine (60 mg, 0.25 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (50 mg, 59%). LCMS (Condition B): tR (1.289 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.00 (d, J = 8.4 Hz, 1H), 7.83 (d, J = 7.6 Hz, 1H), 7.45 – 7.50 (m, 1H), 7.37 – 7.52 (m, 1H), 7.22 (d, J = 2.4 Hz, 1H), 7.10 (d, J = 2.4 Hz, 1H), 6.58 (s, 2H), 3.87 (s, 3H), 3.25 – 3.30 (m, 2H), 2.91 – 2.96 (m, 2H), 2.80 (q, J = 7.2 Hz, 2H), 2.54 (s, 3H), 1.11 (t, J = 7.2 Hz, 3H); HPLC purity: 100% (210 nm). Example 16: Synthesis of 4-(2-(ethyl(methyl)amino)ethyl)naphthalen-2-ol (I-25) Step 1: 4-(2-(ethyl(methyl)amino)ethyl)naphthalen-2-ol trifluoroacetate (I- 25·trifluoroacetate) To a stirred solution of N-ethyl-2-(3-methoxynaphthalen-1-yl)-N-methylethan-1- amine (1.0 g, 4.11 mmol) in CH2Cl2(10 mL) was added 1 M BBr3 in CH2Cl2(5.0 mL) at 0 °C under an atmosphere of nitrogen gas and the reaction was stirred at RT for 2 h. The reaction mixture was then poured into saturated aq. NaHCO3(40 mL) and extracted with 10% MeOH in CH2Cl2(60 mL x 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude material was purified by prep-HPLC to afford the title compound as a brown liquid (100 mg, 11%). LCMS (Condition B): tR (1.077 min) m / z = 230.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 9.80 (s, 1H), 9.57 (br. s, 1H), 7.94 (d, J = 8.4 Hz, 1H), 7.70 (d, J = 7.6 Hz, 1H), 7.38 - 7.42 (m, 1H), 7.30 - 7.35 (m, 1H), 7.03 - 7.05 (m, 2H), 3.17 - 3.27 (m, 6H), 2.84 (s, 3H), 1.21 (t, J = 7.2 Hz, 3H). Step 2: 4-(2-(ethyl(methyl)amino)ethyl)naphthalen-2-ol fumarate (I-25·fumarate) 4-(2-(ethyl(methyl)amino)ethyl)naphthalen-2-ol trifluoroacetate (64 mg, 0.19 mmol) was reformulated as the fumarate salt according to general procedure B which was isolated as a white solid (62 mg, 95%). LCMS (Condition B): tR (1.072 min) m / z = 230.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 9.80 (br. s, 1H), 7.97 (d, J = 8.4 Hz, 1H), 7.72 (d, J = 7.6 Hz, 1H), 7.42 (t, J = 7.2 Hz, 1H), 7.34 - 7.36 (m, 1H), 7.05 - 7.07 (m, 2H), 6.62 (s, 2H), 3.31 - 3.34 (m, 4H), 3.18 - 3.23 (m, 2H), 2.87 (s, 3H), 1.24 (t, J = 7.2 Hz, 3H); HPLC purity: 100% (210 nm). Example 17: Synthesis of N-(2-(3-methoxynaphthalen-1-yl)ethyl)-N-methylpropan- 2-amine (I-18) Step 1: N-(2-(3-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (I-18) To a stirred solution of 2-(3-methoxynaphthalen-1-yl)acetaldehyde (900 mg, 4.5 mmol) in THF (9 mL) was added N-methylpropan-2-amine (0.98 g, 13.5 mmol) and 1-2 drops of acetic acid at RT under an atmosphere of nitrogen gas. After 16 h, NaBH(OAc)3 (2.86 g, 13.5 mmol) was added and the resulting reaction mixture was stirred at RT for 24 h. The reaction mixture was then poured into saturated aq. NaHCO3(100 mL) and extracted with 10 % MeOH in CH2Cl2(100 mL x 3). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure and the residue was purified by reverse phase column chromatography (product eluted at 30% MeCN in water) to afford the title compound as a pale-yellow resin (270 mg, 23%). LCMS (Condition B): tR (1.302 min) m / z = 258.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.02 (d, J = 8.4 Hz, 1H), 7.83 (d, J = 8.0 Hz, 1H), 7.45 - 7.49 (m, 1H), 7.38 - 7.42 (m, 1H), 7.23 (d, J = 2.4 Hz, 1H), 7.13 (d, J = 2.4 Hz, 1H), 3.86 (s, 3H), 3.28 - 3.33 (m, 3H), 3.03 - 3.10 (m, 2H), 2.59 - 2.63 (m, 3H), 1.12 (d, J = 3.6 Hz, 6H); HPLC purity: 100% (210 nm). Step 2: N-(2-(3-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (I- 18·fumarate) N-(2-(3-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (70 mg, 0.27 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as a white solid (80 mg, 79%). LCMS (Condition B): tR (1.307 min) m / z = 258.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.00 (d, J = 8.4 Hz, 1H), 7.82 (d, J = 8.0 Hz, 1H), 7.44 - 7.48 (m, 1H), 7.36 - 7.40 (m, 1H), 7.21 (d, J = 2.4 Hz, 1H), 7.11 (d, J = 2.8 Hz, 1H), 6.55 (s, 2H), 3.86 (s, 3H), 3.19 - 3.27 (m, 3H), 2.88 - 2.92 (m, 2H), 2.49 - 2.51 (m, 3H), 1.07 (d, J = 6.8 Hz, 6H); HPLC purity: 100% (210 nm). Example 18: Synthesis of 4-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol (I- 26) Step 1: 4-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol trifluoroacetate (I- 26·trifluoroacetate) To the stirred solution of N-(2-(3-methoxynaphthalen-1-yl)ethyl)-N-methylpropan- 2-amine (670 mg, 2.62 mmol) in CH2Cl2(6.75 mL) was added 1 M BBr3 in CH2Cl2(3.37 mL) at 0 °C under an atmosphere of nitrogen gas and the reaction was stirred at 0 °C for 2 h. The reaction mixture was then poured on saturated aq. NaHCO3(30 mL) and extracted with 30% MeOH in CH2Cl2(40 mL x 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduce pressure. The crude material was purified by prep-HPLC to afford the title compound as a yellow liquid (420 mg, 66%). LCMS (Condition B): tR (1.129 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 9.80 (s, 1H), 9.48 (s, 1H), 7.97 (d, J = 8.4 Hz, 1H), 7.71 (d, J = 8.0 Hz, 1H), 7.39 - 7.43 (m, 1H), 7.32 - 7.36 (m, 1H), 7.05 – 7.07 (m, 2H), 3.66 - 3.71 (m, 1H), 3.23 - 3.42 (m, 4H), 2.82 – 2.85 (m, 3H), 1.28 (d, J = 6.8 Hz, 3H), 1.22 (d, J = 6.8 Hz, 3H); HPLC purity: 100% (210 nm). Step 2: 4-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol fumarate (I-26·fumarate) 4-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol trifluoroacetate (100 mg, 0.28 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (100 mg, quant.). LCMS (Condition B): tR (1.126 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, MeOD-d4): δ 7.95 (d , J = 8.4 Hz, 1H), 7.70 (d, J = 7.6 Hz, 1H), 7.36 – 7.46 (m, 2H), 7.09 – 7.12 (m, 2H), 6.77 (s, 2H), 3.73 – 3.81 (m, 1H), 3.38 – 3.53 (m, 4H), 2.95 (s, 3H), 1.40 (d, J = 6.8 Hz, 3H), 1.34 (d, J = 6.4 Hz, 3H); HPLC purity: 100% (210 nm). Example 19: Synthesis of 1-(2-(3-methoxynaphthalen-1-yl)ethyl)azetidine (I-20) Step 1: 1-(2-(3-methoxynaphthalen-1-yl)ethyl)azetidine (I-20) To a stirred solution of 2-(3-methoxynaphthalen-1-yl)acetaldehyde (1.0 g, 4.99 mmol) in DCE (10 mL) was added azetidine (1.0 mL, 15.0 mmol) at RT under an atmosphere of nitrogen gas. After 30 min, NaBH(OAc)3 (3.18 g, 15.0 mmol) was added and the reaction was stirred at RT for 24 h. The reaction mixture was then poured into saturated aq. NaHCO3(100 mL) and extracted with 10% MeOH in CH2Cl2(100 mL x 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduce pressure. The crude material was purified by reverse phase column chromatography (product eluted at 10% MeCN in water) to afford the title compound as a pale-yellow resin (140 mg, 12%). LCMS (Condition B): tR (1.237 min) m / z = 242.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 10.63 (br. s, 1H), 8.02 (d, J = 8.0 Hz, 1H), 7.85 (d, J = 8.0 Hz, 1H), 7.48 - 7.51 (m, 1H), 7.40 -7.44 (m, 1H), 7.27 (d, J = 2.4 Hz, 1H), 7.13 (d, J = 2.4 Hz, 1H), 4.00 (t, J = 8.0 Hz, 1H), 3.88 (s, 3H), 3.34 - 3.41 (m, 2H), 3.21 - 3.25 (m, 2H), 2.27 - 2.33 (m, 2H). Step 2: 1-(2-(3-methoxynaphthalen-1-yl)ethyl)azetidine fumarate (I-20·fumarate) 1-(2-(3-methoxynaphthalen-1-yl)ethyl)azetidine (140 mg, 0.58 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (140 mg, 70%). LCMS (Condition B): tR (1.291 min) m / z = 242.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.95 (d, J = 8.0 Hz, 1H), 7.81 (d, J = 8.0 Hz, 1H), 7.46 (t, J = 7.2 Hz, 1H), 7.38 (t, J = 7.2 Hz, 1H), 7.20 (d, J = 2.0 Hz, 1H), 7.06 (d, J = 2.4 Hz, 1H), 6.54 (s, 2H), 3.86 (s, 3H), 3.47 – 3.53 (m, 4H), 3.05 – 3.09 (m, 2H), 2.93 – 2.98 (m, 2H), 2.07 – 2.14 (m, 2H); HPLC purity: 96.6% (210 nm). Example 20: Synthesis of 4-(2-(azetidin-1-yl)ethyl)naphthalen-2-ol (I-28) Step 1: 4-(2-(azetidin-1-yl)ethyl)naphthalen-2-ol (I-28) 4-(2-(azetidin-1-yl)ethyl)naphthalen-2-ol (4 mg, 0.02 mmol) was synthesized analogously to I-10. LCMS (Condition B): tR (1.094 min) m / z = 228.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.93 (d, J = 8.4 Hz, 1H), 7.70 (d, J = 8.0 Hz, 1H), 7.41 (t, J = 7.2 Hz, 1H), 7.30 – 7.35 (m, 1H), 7.02 – 7.07 (m, 2H), 4.08 (t, J = 8.0 Hz, 4H), 3.41 – 3.46 (m, 2H), 3.15 – 3.20 (m, 2H), 2.32 – 2.37 (m, 2H); HPLC purity: 100% (210 nm). Example 21: Synthesis of 1-(2-(3-methoxynaphthalen-1-yl)ethyl)pyrrolidine (I-21) Step 1: 1-(2-(3-methoxynaphthalen-1-yl)ethyl)pyrrolidine trifluoroacetate (I- 21·trifluoroacetate) To a stirred solution of 2-(3-methoxynaphthalen-1-yl) acetaldehyde (500 mg, 2.50 mmol) in DCE (5 mL) was added pyrrolidine (0.63 mL, 7.50 mmol) at RT under an atmosphere of nitrogen gas. After 1 h, NaBH(OAc)3 (1.59 g, 7.49 mmol) was added and the resulting reaction mixture was stirred at RT for 24 h. The reaction mixture was then poured into saturated aq. NaHCO3(100 mL) and extracted with 10% MeOH in CH2Cl2(100 mL x 3). The combined organics were dried over Na2SO4 and concentrated under reduced pressure. The crude material was purified by reverse phase column chromatography (product eluted at 20 % MeCN in water) to afford the title compound as a yellow resin (97 mg, 15%). LCMS (Condition B): tR (1.255 min) m / z = 256.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 9.80 (br. s, 1H), 8.01 (d, J = 8.4 Hz, 1H), 7.85 (d, J = 8.0 Hz, 1H), 7.50 (t, J = 7.2 Hz, 1H), 7.42 (t, J = 7.2, 1H), 7.27 (d, J = 2.4 Hz, 1H), 7.15 (d, J = 2.4 Hz, 1H), 3.86 (s, 3H), 3.63 - 3.65 (m, 2H), 3.37 – 3.46 (m, 4H), 3.10 - 3.15 (m, 2H), 2.04 - 2.06 (m, 2H), 1.88 - 1.91 (m, 2H). Step 2: 1-(2-(3-methoxynaphthalen-1-yl)ethyl)pyrrolidine fumarate (I-21·fumarate) 1-(2-(3-methoxynaphthalen-1-yl)ethyl)pyrrolidine trifluoroacetate (70 mg, 0.19 mmol) was reformulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (64 mg, 94%). LCMS (Condition B): tR (1.283 min) m / z = 256.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.02 (d, J = 8.4 Hz, 1H), 7.86 (d, J = 8.0 Hz, 1H), 7.48 – 7.53 (m, 1H), 7.41 – 7.46 (m, 1H), 7.28 (d, J = 2.4 Hz, 1H), 7.15 (d, J = 2.4 Hz, 1H), 6.63 (s, 2H), 3.88 (s, 3H), 3.35 – 3.63 (m, 8H), 1.90 – 2.05 (m, 4H); HPLC purity: 100% (210 nm). Example 22: Synthesis of 4-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol (I-29) Step 1: 4-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol trifluoroacetate (I-29·trifluoroacetate) To a stirred solution of 1-(2-(3-methoxynaphthalen-1-yl)ethyl)pyrrolidine (470 mg, 1.84 mmol) in CH2Cl2(4.7 mL) was added 1 M BBr3 in CH2Cl2(2.35 mL) at 0 °C under an atmosphere of nitrogen gas and the reaction mixture was stirred at 0 °C for 2 h. The reaction mixture was then poured into saturated aq. NaHCO3(25 mL) and extracted with 30% MeOH in CH2Cl2(45 mL x 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduced pressure and the crude material was purified by prep-HPLC to afford the title compound as a pale-yellow liquid (200 mg, 31%). LCMS (Condition B): tR (1.089 min) m / z = 242.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 9.88 (br. s, 1H), 9.83 (s, 1H), 7.97 (d, J = 8.4 Hz, 1H), 7.72 (d, J = 8.0 Hz, 1H), 7.42 (t, J = 7.2 Hz, 1H), 7.32 - 7.36 (m, 1H), 7.05 - 7.08 (m, 2H), 3.62 - 3.71 (m, 2H), 3.31 - 3.46 (m, 4H), 3.11 - 3.16 (m, 2H), 2.05 - 2.09 (m, 2H), 1.89 - 1.94 (m, 2H). Step 2: 4-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol fumarate (I-29·fumarate) 4-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol trifluoroacetate (160 mg, 0.45 mmol) was reformulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (100 mg, 88%). LCMS (Condition B): tR (1.125 min) m / z = 242.2 [M+H]+;1H NMR (400 MHz, MeOD-d4): δ 7.97 (d, J = 8.4 Hz, 1H), 7.71 (d, J = 8.0 Hz, 1H), 7.37 – 7.47 (m, 2H), 7.11 (s, 2H), 6.79 (s, 2H), 3.69 – 3.85 (m, 2H), 3.54 – 3.60 (m, 2H), 3.47 – 3.53 (m, 2H), 3.11 – 3.29 (m, 2H), 2.02 – 2.27 (m, 4H); HPLC purity: 100% (210 nm). Example 23: Synthesis of 2-(4-methoxynaphthalen-1-yl)-N,N-dimethylethan-1- amine (I-68) Step 1: 1-methoxy-4-(2-nitrovinyl)naphthalene (20) To a solution of 4-methoxy-1-naphthaldehyde (4.05 g, 21.7 mmol) in nitromethane (50 mL, 934 mmol) was added ammonium acetate (4.53 g, 58.7 mmol) and the mixture was stirred at 80 °C for 3 h under a N2 atmosphere. After cooling, the reaction was diluted with H2O (80 mL) and left to stand at 0 °C overnight. The mixture was filtered, and the filtered solids were washed with H2O and dried to afford the target product as orange crystals (3.03 g, 61%).1H NMR (400 MHz, CDCl3): δ 8.80 (d, J = 13.3 Hz, 1H), 8.35 (ddd, J = 8.4, 1.5, 0.7 Hz, 1H), 8.13 (dt, J = 8.6, 0.9 Hz, 1H), 7.78 (d, J = 8.2 Hz, 1H), 7.67 (ddd, J = 8.5, 7.0, 1.4 Hz, 1H), 7.66 (d, J = 13.5 Hz, 1H), 7.58 (ddd, J = 8.2, 6.9, 1.2 Hz, 1H), 6.88 (d, J = 8.2 Hz, 1H), 4.08 (s, 3H). Step 2: 2-(4-methoxynaphthalen-1-yl)ethan-1-amine (21) A solution of 1-methoxy-4-(2-nitrovinyl)naphthalene (1.42 g, 6.19 mmol) in anhydrous THF (30 mL) was cooled to 0 °C and LiAlH4 (943 mg, 24.8 mmol) was added portionwise under nitrogen atmosphere. The mixture was refluxed for 3 h and then, after cooling, was quenched with cold H2O (1 mL), then 15% aq. NaOH (1 mL), then H2O (3 mL). The resulting mixture was filtered through a pad of celite and the filter cake washed with THF (3 x 25 mL). The filtrate was concentrated under reduced pressure and the residue purified by flash chromatography (SiO2, 2-10% MeOH-NH3in CH2Cl2) to provide the title compound as a clear oil (328 mg, 26%).1H NMR (400 MHz, DMSO- d6) δ 8.17 (dd, J = 8.2, 1.5 Hz, 1H), 8.04 (d, J = 8.4 Hz, 1H), 7.55 (ddd, J = 8.4, 6.8, 1.5 Hz, 1H), 7.48 (ddd, J = 8.2, 6.8, 1.3 Hz, 1H), 7.26 (d, J = 7.8 Hz, 1H), 6.88 (d, J = 7.9 Hz, 1H), 3.94 (s, 3H), 3.05 – 2.99 (m, 1H), 2.81 (dd, J = 8.2, 6.6 Hz, 2H). Step 3: 2-(4-methoxynaphthalen-1-yl)-N,N-dimethylethan-1-amine (I-68) To a solution of 2-(4-methoxynaphthalen-1-yl)ethan-1-amine (141 mg, 0.70 mmol) in MeOH (2.0 mL) at 0 °C was added 40% formaldehyde (158 mg, 2.10 mmol) and NaCNBH3(176 mg, 2.80 mmol) and the mixture was stirred at room temperature for 3 hours. The mixture was then concentrated under a stream of nitrogen and treated with 1 M NaOH (3.0 mL) and extracted with EtOAc (3 x 10 mL). The pooled organics were washed with brine (10 mL), dried over anhydrous MgSO4 and concentrated under reduced pressure to give a yellow oil which was purified by column chromatography (SiO2, 5% MeOH-NH3in CH2Cl2) to provide 2-(4-methoxynaphthalen-1-yl)-N,N- dimethylethan-1-amine (75 mg, 47%) as a yellow oil.1H NMR (400 MHz, CDCl3) δ 8.30 (ddd, J = 8.3, 1.5, 0.7 Hz, 1H), 7.98 (dt, J = 8.4, 0.8 Hz, 1H), 7.54 (ddd, J = 8.4, 6.8, 1.5 Hz, 1H), 7.47 (ddd, J = 8.1, 6.8, 1.3 Hz, 1H), 7.25 (d, J = 7.9 Hz, 1H), 6.74 (d, J = 7.8 Hz, 1H), 3.98 (s, 3H), 3.24 – 3.15 (m, 2H), 2.69 – 2.60 (m, 2H), 2.39 (s, 6H). Step 4: 2-(4-methoxynaphthalen-1-yl)-N,N-dimethylethan-1-amine fumarate (I- 68·fumarate) 2-(4-methoxynaphthalen-1-yl)-N,N-dimethylethan-1-amine was formulated as the fumarate salt according to general procedure B and was isolated as white crystals (37 mg, 22%).1H NMR (400 MHz, DMSO-d6) δ 8.20 (dd, J = 8.3, 1.0 Hz, 1H), 8.06 (d, J = 8.2 Hz, 1H), 7.58 (ddd, J = 8.4, 6.8, 1.5 Hz, 1H), 7.51 (ddd, J = 8.1, 6.8, 1.2 Hz, 1H), 7.34 (d, J = 7.9 Hz, 1H), 6.91 (d, J = 7.9 Hz, 1H), 6.57 (s, 2H), 3.95 (s, 3H), 3.31 – 3.23 (m, 2H), 3.03 – 2.94 (m, 2H), 2.64 (s, 6H).1H qNMR purity: 96.0% (ERETIC). Example 24: Synthesis of 4-(2-(dimethylamino)ethyl)naphthalen-1-ol (I-69) Step 1: 4-(2-(dimethylamino)ethyl)naphthalen-1-ol (I-69) To a solution of 2-(4-methoxynaphthalen-1-yl)-N,N-dimethylethan-1-amine (47 mg, 0.20 mmol) in CH2Cl2(3.0 mL) at 0 °C was added BBr3 (0.4 mL, 4.28 mmol) and the mixture was stirred at 0 °C for 1.5 hours. The reaction was diluted with CH2Cl2(20 mL), cooled to 0 °C, and treated with saturated aq. Na2CO3 (2.0 mL) dropwise followed by 2.5 M aq. NaOH (4.0 mL). The CH2Cl2was evaporated under a stream of nitrogen gas and the remaining aqueous phase was extracted with EtOAc (3 x 20 mL). The combined organics were washed with brine (15 mL), dried over anhydrous MgSO4, filtered and concentrated under reduced pressure. The crude material was purified by flash chromatography (SiO2, 2-10% MeOH-NH3in CH2Cl2) to afford 4-(2- (dimethylamino)ethyl)naphthalen-1-ol (28 mg, 65%) as a colourless solid. Step 2: 4-(2-(dimethylamino)ethyl)naphthalen-1-ol fumarate (I-69·fumarate) 4-(2-(dimethylamino)ethyl)naphthalen-1-ol (28 mg, 0.13 mmol) was formulated as the fumarate salt according to general procedure B and was isolated as white crystals (22 mg, 51%). LCMS (Condition A): tR (4.853) m / z = 230.15 [M+H]+;1H NMR (400 MHz, DMSO-d6) δ 10.26 (br s, 1H), 8.17 (ddd, J = 8.3, 1.5, 0.6 Hz, 1H), 8.02 – 7.95 (m, 1H), 7.52 (ddd, J = 8.4, 6.7, 1.5 Hz, 1H), 7.45 (ddd, J = 8.0, 6.7, 1.2 Hz, 1H), 7.19 (d, J = 7.7 Hz, 1H), 6.80 (d, J = 7.7 Hz, 1H), 6.56 (s, 2H), 3.24 – 3.15 (m, 2H), 2.92 – 2.83 (m, 2H), 2.56 (s, 6H);13C NMR (101 MHz, DMSO-d6) δ 167.3, 152.2, 134.7, 132.4, 127.1, 126.3, 125.0, 124.5, 124.2, 123.4, 122.7, 107.6, 58.5, 43.3, 28.2;1H qNMR purity: 99.6% (ERETIC). Example 25: Synthesis of N-ethyl-2-(4-methoxynaphthalen-1-yl)-N-methylethan-1- amine (I-78) Step 1: 1-methoxy-4-(2-methoxyvinyl)naphthalene (22) A suspension of methoxymethyltriphenylphosphonium chloride (8.1 g, 23.6 mmol) in anhydrous THF (70 mL) at 0 °C was treated with KOtBu (3.62 g, 32.2 mmol) portionwise and the mixture was stirred for 20 min at RT. A solution of 4-methoxy-1- naphthaldehyde (4.0 g, 21.5 mmol) in THF (10 mL) was added and the reaction was stirred at rt for 20 min. The reaction was quenched with sat. aq. NH4Cl (20 mL) and the organic layer was separated, dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by flash chromatography (SiO2, 0-20% EtOAc in hexane) to provide the title compound as a mixture of trans and cis isomers (depicted as a crossed double bond in the scheme above) which was a light yellow oil (3.99 g, 87%).1H NMR (400 MHz, CDCl3): δ trans 8.31 – 8.26 (m, 1H), 8.04 – 8.00 (m, 1H), 7.56 – 7.51 (m, 1H), 7.51 – 7.47 (m, 1H), 7.32 (dd, J = 7.9, 0.9 Hz, 1H), 6.88 (d, J = 12.6 Hz, 1H), 6.77 (d, J = 7.9 Hz, 1H), 6.38 (dd, J = 12.6, 0.9 Hz, 1H), 4.00 (s, 3H), 3.78 (s, 3H); cis 8.06 – 8.02 (m, 1H), 7.94 (d, J = 8.1 Hz, 1H), 7.52 – 7.44 (m, 3H), 6.83 (d, J = 8.1 Hz, 1H), 6.31 (d, J = 7.1 Hz, 1H), 5.82 (d, J = 7.1 Hz, 1H), 4.00 (s, 3H), 3.77 (s, 3H). Step 2: 2-(4-methoxynaphthalen-1-yl)acetaldehyde (23) A solution of 1-methoxy-4-(2-methoxyvinyl)naphthalene (3.98 g, 18.6 mmol) in THF (40 mL) and 2 M aq. HCl (30 mL) was stirred at 90 °C for 3.5 h. The reaction mixture was cooled in an ice bath and quenched with NaHCO3. Et2O (40 mL) was added and the organic layer was separated, dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by flash chromatography (SiO2, 0-20% EtOAc in hexane) to provide 2-(4-methoxynaphthalen-1- yl)acetaldehyde as a bright yellow oil (2.97 g, 80%).1H NMR (400 MHz, CDCl3): δ 9.75 (t, J = 2.5 Hz, 1H), 8.34 (ddd, J = 8.0, 1.7, 0.7 Hz, 1H), 7.80 (ddd, J = 8.4, 1.5, 0.7 Hz, 1H), 7.56 (ddd, J = 8.4, 6.8, 1.7 Hz, 1H), 7.52 (ddd, J = 8.2, 6.8, 1.5 Hz, 1H), 7.31 (dt, J = 7.8, 0.7 Hz, 1H), 6.81 (d, J = 7.8 Hz, 1H), 4.01 (s, 3H), 4.01 (dd, J = 2.4, 0.7 Hz, 2H). Step 3: N-ethyl-2-(4-methoxynaphthalen-1-yl)-N-methylethan-1-amine (I-78) A stirred mixture of N-methylethylamine (0.21 mL, 2.50 mmol) in CH2Cl2(5 mL) at 0 °C was treated with NaBH(OAc)3 (529 mg, 2.50 mmol) and then with a solution of 2-(4-methoxynaphthalen-1-yl)acetaldehyde (250 mg, 1.25 mmol) in CH2Cl2(5 mL) and the mixture was stirred overnight at RT. The reaction was quenched by addition of 15% aq. NaOH (2 mL), diluted with water (20 mL) and extracted with CH2Cl2(3 x 15 mL). The combined organics were washed with brine (15 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude material was purified by flash chromatography (SiO2, 0-10% MeOH-NH3in CH2Cl2) to provide N-ethyl-2-(4- methoxynaphthalen-1-yl)-N-methylethan-1-amine (271 mg, 89%) as a colourless oil which slowly formed colourless crystals.1H NMR (400 MHz, CDCl3): δ 8.30 (ddd, J = 8.3, 1.5, 0.7 Hz, 1H), 7.99 (ddd, J = 8.3, 1.3, 0.7 Hz, 1H), 7.54 (ddd, J = 8.4, 6.8, 1.5 Hz, 1H), 7.47 (ddd, J = 8.2, 6.8, 1.3 Hz, 1H), 7.25 (d, J = 7.8 Hz, 1H), 6.74 (d, J = 7.8 Hz, 1H), 3.98 (s, 3H), 3.23 – 3.15 (m, 2H), 2.75 – 2.67 (m, 2H), 2.57 (q, J = 7.2 Hz, 2H), 2.41 (s, 3H), 1.13 (t, J = 7.2 Hz, 3H). Step 4: N-ethyl-2-(4-methoxynaphthalen-1-yl)-N-methylethan-1-amine fumarate (I- 78·fumarate) N-ethyl-2-(4-methoxynaphthalen-1-yl)-N-methylethan-1-amine (92 mg, 0.38 mmol) was formulated as the fumarate salt according to general procedure B which was collected as white crystals (120 mg, 76%).1H NMR (400 MHz, DMSO-d6): δ 8.19 (dd, J = 8.4, 1.5 Hz, 1H), 8.06 (d, J = 8.4 Hz, 1H), 7.58 (ddd, J = 8.4, 6.8, 1.5 Hz, 1H), 7.51 (ddd, J = 8.1, 6.8, 1.2 Hz, 1H), 7.35 (d, J = 7.8 Hz, 1H), 6.91 (d, J = 7.9 Hz, 1H), 6.56 (s, 2H), 3.95 (s, 3H), 3.32 – 3.24 (m, 2H), 3.04 – 2.98 (m, 2H), 2.94 (q, J = 7.2 Hz, 2H), 2.64 (s, 3H), 1.15 (t, J = 7.2 Hz, 3H);13C NMR (101 MHz, DMSO-d6): δ 167.1, 154.0, 134.7, 132.1, 127.0, 126.8, 126.0, 125.2, 125.1, 123.6, 122.2, 104.1, 55.8, 55.6, 50.0, 39.1, 27.5, 10.0;1H qNMR purity: 100% (ERETIC). Example 26: Synthesis of 4-(2-(ethyl(methyl)amino)ethyl)naphthalen-1-ol (I-70) Step 1: 4-(2-(ethyl(methyl)amino)ethyl)naphthalen-1-ol (I-70) A solution of N-ethyl-2-(4-methoxynaphthalen-1-yl)-N-methylethan-1-amine (174 mg, 0.72 mmol) in CH2Cl2(5 mL) at 0 °C was treated with BBr3 (0.34 mL, 3.58 mmol) and the mixture stirred at 0 °C for 1.5 h. The reaction was diluted with CH2Cl2(15 mL) and cooled to 0 °C before being quenched with sat. aq. Na2CO3 (1 mL). The mixture was diluted with water (15 mL) and adjusted to pH ~12 with 15% aq. NaOH. The phases were separated and the aqueous was extracted with EtOAc (3 x 15 mL). The combined organics were washed with brine (15 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude material was purified by flash chromatography (SiO2, 0-10% MeOH-NH3in CH2Cl2) to provide 4-(2- (ethyl(methyl)amino)ethyl)naphthalen-1-ol (96 mg, 59%) as a light brown solid.1H NMR (400 MHz, CDCl3): δ 8.32 – 8.26 (m, 1H), 8.01 – 7.92 (m, 1H), 7.53 – 7.41 (m, 2H), 7.11 (d, J = 7.6 Hz, 1H), 6.70 (d, J = 7.6 Hz, 1H), 4.14 (br. s, 1H), 3.26 – 3.18 (m, 2H), 2.82 – 2.73 (m, 2H), 2.66 (q, J = 7.2 Hz, 2H), 2.47 (s, 3H), 1.17 (t, J = 7.2 Hz, 3H). Step 2: 4-(2-(ethyl(methyl)amino)ethyl)naphthalen-1-ol fumarate (I-70·fumarate) 4-(2-(ethyl(methyl)amino)ethyl)naphthalen-1-ol (90 mg, 0.39 mmol) was formulated as the fumarate salt according to general procedure B which was collected as a pale brown solid (101 mg, 86%).1H NMR (400 MHz, DMSO-d6): δ 10.14 (br. s, 1H), 8.16 (dd, J = 8.3, 1.4 Hz, 1H), 7.97 (d, J = 8.4 Hz, 1H), 7.52 (ddd, J = 8.4, 6.7, 1.5 Hz, 1H), 7.48 – 7.40 (m, 1H), 7.19 (d, J = 7.7 Hz, 1H), 6.80 (d, J = 7.6 Hz, 1H), 6.53 (s, 2H), 3.21 – 3.12 (m, 2H), 2.86 – 2.79 (m, 2H), 2.75 (q, J = 7.2 Hz, 2H), 2.49 (s, 3H), 1.09 (t, J = 7.2 Hz, 3H);13C NMR (101 MHz, DMSO-d6): δ 167.8, 152.2, 135.1, 132.4, 127.1, 126.3, 125.1, 125.0, 124.3, 123.4, 122.7, 107.6, 56.8, 50.2, 28.3, 25.5, 20.8;1H qNMR purity: 96.8% (ERETIC). Example 27: Synthesis of N-(2-(4-methoxynaphthalen-1-yl)ethyl)-N-methylpropan- 2-amine (I-79) Step 1: N-(2-(4-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (I-79) A stirred mixture of N-methyl(isopropyl)amine (0.26 mL, 2.50 mmol) in CH2Cl2(5 mL) at 0 °C was treated with NaBH(OAc)3 (529 mg, 2.50 mmol) and then with a solution of 2-(4-methoxynaphthalen-1-yl)acetaldehyde (250 mg, 1.25 mmol) in CH2Cl2(5 mL) and the mixture was stirred overnight at room temperature. The reaction was quenched by addition of 15% aq. NaOH (2 mL), diluted with water (20 mL) and extracted with CH2Cl2(3 x 15 mL). The combined organics were washed with brine (15 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude material was purified by flash chromatography (SiO2, 0-10% MeOH-NH3in CH2Cl2) to provide N-(2- (4-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (286 mg, 89%) as a colourless oil.1H NMR (400 MHz, CDCl3): δ 8.30 (ddd, J = 8.3, 1.5, 0.7 Hz, 1H), 8.00 (ddd, J = 8.4, 1.3, 0.7 Hz, 1H), 7.54 (ddd, J = 8.4, 6.8, 1.5 Hz, 1H), 7.47 (ddd, J = 8.2, 6.8, 1.3 Hz, 1H), 7.26 (d, J = 7.8 Hz, 1H), 6.75 (d, J = 7.8 Hz, 1H), 3.98 (s, 3H), 3.22 – 3.14 (m, 2H), 2.96 (hept, J = 6.6 Hz, 1H), 2.76 – 2.67 (m, 2H), 2.41 (s, 3H), 1.05 (d, J = 6.6 Hz, 6H). Step 2: N-(2-(4-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine fumarate (I- 79·fumarate) N-(2-(4-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (75 mg, 0.29 mmol) was formulated as the fumarate salt according to general procedure B which was collected as white crystals (92 mg, 73%).1H NMR (400 MHz, DMSO-d6): δ 8.19 (dd, J = 8.4, 1.5 Hz, 1H), 8.07 (d, J = 8.4 Hz, 1H), 7.58 (ddd, J = 8.4, 6.7, 1.5 Hz, 1H), 7.51 (ddd, J = 8.1, 6.8, 1.2 Hz, 1H), 7.36 (d, J = 7.9 Hz, 1H), 6.92 (d, J = 7.9 Hz, 1H), 6.56 (s, 3H), 3.95 (s, 3H), 3.41 (h, J = 6.6 Hz, 1H), 3.34 – 3.25 (m, 2H), 3.05 – 2.97 (m, 2H), 2.62 (s, 3H), 1.15 (d, J = 6.6 Hz, 6H);13C NMR (101 MHz, DMSO-d6): δ 167.2, 154.0, 134.7, 132.1, 127.1, 126.8, 126.0, 125.2, 125.1, 123.6, 122.2, 104.1, 55.6, 54.7, 53.2, 34.7, 27.9, 16.4;1H qNMR purity: 100% (ERETIC). Example 28: Synthesis of 4-(2-(isopropyl(methyl)amino)ethyl)naphthalen-1-ol (I- 71) Step 1: 4-(2-(isopropyl(methyl)amino)ethyl)naphthalen-1-ol (I-71) A solution of N-(2-(4-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (206 mg, 0.80 mmol) in CH2Cl2(5 mL) at 0 °C was treated with BBr3 (0.38 mL, 4.00 mmol) and the mixture stirred at 0 °C for 1.5 h. The reaction was diluted with CH2Cl2(15 mL) and cooled to 0 °C before being quenched with sat. aq. Na2CO3 (1 mL). The mixture was diluted with water (15 mL) and adjusted to pH ~12 with 15% aq. NaOH. The phases were separated and the aqueous was extracted with EtOAc (3 x 15 mL). The combined organics were washed with brine (15 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude material was purified by flash chromatography (SiO2, 0-10% MeOH-NH3in CH2Cl2) to provide 4-(2- (isopropyl(methyl)amino)ethyl)naphthalen-1-ol (135 mg, 69%) as a light brown solid.1H NMR (400 MHz, CDCl3): δ 8.35 – 8.24 (m, 1H), 8.00 – 7.93 (m, 1H), 7.54 – 7.41 (m, 2H), 7.11 (d, J = 7.6 Hz, 1H), 6.76 (d, J = 7.6 Hz, 1H), 4.42 (br. s, 1H), 3.31 – 3.23 (m, 2H), 3.17 (hept, J = 6.7 Hz, 1H), 2.88 – 2.79 (m, 2H), 2.49 (s, 3H), 1.15 (d, J = 6.6 Hz, 6H). Step 2: 4-(2-(isopropyl(methyl)amino)ethyl)naphthalen-1-ol fumarate (I-71·fumarate) 4-(2-(isopropyl(methyl)amino)ethyl)naphthalen-1-ol (115 mg, 0.47 mmol) was formulated as the fumarate salt according to general procedure B which was collected as a brown powder (115 mg, 35%).1H NMR (400 MHz, DMSO-d6): δ 10.10 (br. s, 1H), 8.18 (dd, J = 8.3, 1.5 Hz, 1H), 8.03 (d, J = 8.4 Hz, 1H), 7.54 (ddd, J = 8.4, 6.7, 1.5 Hz, 1H), 7.46 (ddd, J = 8.1, 6.8, 1.2 Hz, 1H), 7.24 (d, J = 7.7 Hz, 1H), 6.81 (d, J = 7.7 Hz, 1H), 6.59 (s, 2H), 3.57 (h, J = 6.6 Hz, 1H), 3.35 – 3.26 (m, 2H), 3.16 – 3.08 (m, 2H), 2.72 (s, 3H), 1.20 (d, J = 6.6 Hz, 6H);13C NMR (101 MHz, DMSO-d6): δ 166.6, 152.6, 134.4, 132.4, 127.5, 126.5, 125.0, 124.5, 123.43, 123.38, 122.8, 107.6, 55.4, 53.1, 34.4, 27.3, 16.1;1H qNMR purity: 97.3% (ERETIC). Example 29: Synthesis of 1-(2-(4-methoxynaphthalen-1-yl)ethyl)pyrrolidine (I-I-81) Step 1: 1-(2-(4-methoxynaphthalen-1-yl)ethyl)pyrrolidine (I-81) A stirred mixture of pyrrolidine (0.21 mL, 2.50 mmol) in CH2Cl2(5 mL) at 0 °C was treated with NaBH(OAc)3 (529 mg, 2.50 mmol) and then with a solution of 2-(4- methoxynaphthalen-1-yl)acetaldehyde (250 mg, 1.25 mmol) in CH2Cl2(5 mL) and the mixture was stirred overnight at room temperature. The reaction was quenched by addition of 15% aq. NaOH (2 mL), diluted with water (20 mL) and extracted with CH2Cl2(3 x 15 mL). The combined organics were washed with brine (15 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude material was purified by flash chromatography (SiO2, 0-10% MeOH-NH3in CH2Cl2) to provide 1-(2- (4-methoxynaphthalen-1-yl)ethyl)pyrrolidine (302 mg, 95%) as a light yellow oil which slowly solidified.1H NMR (400 MHz, CDCl3): δ 8.30 (ddd, J = 8.2, 1.6, 0.7 Hz, 1H), 8.02 (ddd, J = 8.4, 1.2, 0.7 Hz, 1H), 7.53 (ddd, J = 8.4, 6.8, 1.5 Hz, 1H), 7.47 (ddd, J = 8.2, 6.8, 1.3 Hz, 1H), 7.26 (d, J = 7.8 Hz, 1H), 6.74 (d, J = 7.8 Hz, 1H), 3.98 (s, 3H), 3.30 – 3.20 (m, 2H), 2.85 – 2.76 (m, 2H), 2.72 – 2.62 (m, 4H), 1.90 – 1.81 (m, 4H). Step 2: 1-(2-(4-methoxynaphthalen-1-yl)ethyl)pyrrolidine fumarate (I-81·fumarate) 1-(2-(4-methoxynaphthalen-1-yl)ethyl)pyrrolidine (101 mg, 0.40 mmol) was formulated as the fumarate salt according to general procedure B which was collected as a white powder (137 mg, 81%).1H NMR (400 MHz, DMSO-d6): δ 8.19 (dd, J = 8.2, 1.5 Hz, 1H), 8.07 (d, J = 8.4 Hz, 1H), 7.58 (ddd, J = 8.4, 6.8, 1.5 Hz, 1H), 7.51 (ddd, J = 8.1, 6.8, 1.2 Hz, 1H), 7.35 (d, J = 7.9 Hz, 1H), 6.91 (d, J = 7.9 Hz, 1H), 6.56 (s, 2H), 3.95 (s, 3H), 3.35 – 3.26 (m, 2H), 3.17 – 3.09 (m, 6H), 1.95 – 1.83 (m, 4H);13C NMR (101 MHz, DMSO-d6): δ 167.3, 154.0, 134.7, 132.0, 127.0, 126.8, 125.9, 125.22, 125.15, 123.6, 122.2, 104.0, 55.6, 55.0, 52.9, 29.0, 22.9;1H qNMR purity: 99.6% (ERETIC). Example 30: Synthesis of 4-(2-(pyrrolidin-1-yl)ethyl)naphthalen-1-ol (I-75) Step 1: 4-(2-(pyrrolidin-1-yl)ethyl)naphthalen-1-ol (I-75) A solution of 1-(2-(4-methoxynaphthalen-1-yl)ethyl)pyrrolidine (200 mg, 0.78 mmol) in CH2Cl2(5 mL) at 0 °C was treated with BBr3 (0.37 mL, 3.92 mmol) and the mixture stirred at 0 °C for 1.5 h. The reaction was diluted with CH2Cl2(15 mL) and cooled to 0 °C before being quenched with sat. aq. Na2CO3 (1 mL). The mixture was diluted with water (15 mL) and adjusted to pH ~12 with 15% aq. NaOH. The phases were separated and the aqueous was extracted with EtOAc (3 x 15 mL). The combined organics were washed with brine (15 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude material was purified by flash chromatography (SiO2, 0-10% MeOH-NH3in CH2Cl2) to provide 4-(2-(pyrrolidin-1- yl)ethyl)naphthalen-1-ol (40 mg, 21%) as a light red resin.1H NMR (400 MHz, CDCl3): δ 8.30 – 8.21 (m, 1H), 8.01 – 7.94 (m, 1H), 7.52 – 7.40 (m, 2H), 7.12 (d, J = 7.6 Hz, 1H), 6.70 (d, J = 7.6 Hz, 1H), 3.30 – 3.21 (m, 2H), 2.90 – 2.81 (m, 2H), 2.79 – 2.71 (m, 4H), 2.37 (br. s, 1H), 1.93 – 1.85 (m, 4H). Step 2: 4-(2-(pyrrolidin-1-yl)ethyl)naphthalen-1-ol fumarate (I-75·fumarate) 4-(2-(pyrrolidin-1-yl)ethyl)naphthalen-1-ol (29 mg, 0.12 mmol) was formulated as the fumarate salt according to general procedure B which was collected as a light pink solid (29 mg, 79%).1H NMR (400 MHz, DMSO-d6): δ 10.07 (br. s, 1H), 8.16 (dd, J = 8.3, 1.4 Hz, 1H), 7.97 (d, J = 8.4 Hz, 1H), 7.52 (ddd, J = 8.4, 6.7, 1.5 Hz, 1H), 7.44 (ddd, J = 8.0, 6.7, 1.1 Hz, 1H), 7.19 (d, J = 7.7 Hz, 1H), 6.79 (d, J = 7.7 Hz, 1H), 6.51 (s, 2H), 3.17 (dd, J = 9.9, 6.4 Hz, 2H), 2.90 (dd, J = 10.0, 6.2 Hz, 2H), 2.87 – 2.78 (m, 4H), 1.86 – 1.73 (m, 4H);13C NMR (101 MHz, DMSO-d6): δ 167.7, 152.1, 135.0, 132.4, 127.0, 126.3, 125.2, 125.0, 124.3, 123.5, 122.7, 107.6, 56.1, 53.3, 30.2, 23.0;1H qNMR purity: 98.5% (ERETIC). Example 31: Synthesis of 2-(4-fluoronaphthalen-1-yl)ethan-1-amine (I-76) Step 1: (E)-1-fluoro-4-(2-nitrovinyl)naphthalene (25) A solution of 4-fluoro-1-naphthaldehyde (2.0 g, 11.5 mmol) and ammonium acetate (443 mg, 0.5 equiv., 5.74 mmol) in nitromethane (6.15 mL, 10 equiv., 115.0 mmol) was stirred at reflux under a CaCl2 trap for 16 h. The reaction was cooled to RT and quenched with water (5 mL). The resulting precipitate was collected by vacuum filtration, washed with water with maceration, and then washed with hexane to afford a brown solid. The brown solid was dissolved in CH2Cl2, concentrated under a stream of nitrogen gas, and then recrystallised from EtOH with a few drops of water to afford the title compound as brown needles (1.42 g, 57%).1H NMR (400 MHz, DMSO-d6) δ 8.78 (d, J = 13.3 Hz, 1H), 8.37 (dd, J = 7.9, 1.6 Hz, 1H), 8.24 (d, J = 13.1 Hz, 1H), 8.15 (ddd, J = 8.1, 3.1, 1.9 Hz, 2H), 7.83 – 7.66 (m, 2H), 7.47 (dd, J = 10.4, 8.2 Hz, 1H).13C NMR (101 MHz, DMSO-d6) δ 160.2 (d, J = 257.2 Hz), 139.4, 134.7, 132.7 (d, J = 5.3 Hz), 128.9, 128.1 (d, J = 9.4 Hz), 127.5, 123.7 (d, J = 2.7 Hz), 123.4 (d, J = 4.4 Hz), 123.0 (d, J = 16.3 Hz), 120.7 (d, J = 5.6 Hz), 110.1 (d, J = 20.8 Hz). Step 2: 2-(4-fluoronaphthalen-1-yl)ethan-1-amine acetate (26) To ice-cold anhydrous THF (100 mL) was added LiAlH4 (1.14 g, 29.9 mmol) in portions, followed by (E)-1-fluoro-4-(2-nitrovinyl)naphthalene (1.3 g, 6.0 mmol) dissolved in minimal anhydrous THF at a rate that maintained a gentle effervescence. The resulting suspension was then refluxed under N2 gas for 16 h. The cooled reaction was then quenched with water (1.2 mL), 3.75 M aq. NaOH (1.2 mL), and water (3.6 mL) and stirred with anhydrous Na2SO4for 30 min. The suspension was then filtered through a celite pad under vacuum and the filter cake was eluted with hot THF (50 mL x 3). The combined filtrate was concentrated in vacuo and the residue was taken up in EtOAc and water (1:1, 100 mL) and then 35% w / w aq. HCl was added until the aqueous layer was acidic. The layers were separated and the organic layer was further extracted with 1 M aq. HCl (20 mL x 2). The pH of the combined aqueous layer was adjusted to 9-10 with saturated aq. Na2CO3 and then extracted with CH2Cl2(50 mL x 3). The combined CH2Cl2layer was washed with brine (50 mL), dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was crystallised with EtOAc:hexane to afford the title compound as off-white crystals as the acetate salt (225 mg, 15%).1H NMR (400 MHz, DMSO-d6) δ 8.22 – 8.14 (m, 1H), 8.11 – 8.03 (m, 1H), 7.72 – 7.57 (m, 2H), 7.36 (dd, J = 7.8, 5.7 Hz, 1H), 7.25 (dd, J = 10.8, 7.9 Hz, 1H), 3.25 – 3.15 (m, 2H), 2.97 – 2.85 (m, 2H), 1.80 (s, 3H).13C NMR (101 MHz, DMSO-d6) δ 173.4, 156.9 (d, J = 248.1 Hz), 132.6 (d, J = 4.4 Hz), 131.7 (d, J = 4.3 Hz), 127.2, 126.5, 126.4, 124.2 (d, J = 2.8 Hz), 123.1 (d, J = 16.1 Hz), 120.4 (d, J = 5.5 Hz), 109.2 (d, J = 19.3 Hz), 41.5, 33.7, 23.0. Step 3: 2-(4-fluoronaphthalen-1-yl)-N,N-dimethylethan-1-amine (I-76) To a solution of 2-(4-fluoro-1-naphthyl)ethylamine (200 mg, 1.06 mmol) in (CH2Cl)2(5 mL) was added sodium triacetoxyborohydride (900 mg, 4.23 mmol) and then aqueous formaldehyde (37% w / w, 0.2 mL, 7.26 mmol) at RT. The reaction was stirred at RT for 1 h, and then quenched with saturated aq. NaHCO3(25 mL) and diluted with 50 mL of CH2Cl2. The layers were separated and the aqueous layer was further extracted with CH2Cl2(50 mL x 2). The combined organic layer was washed with water (50 mL), then brine (50 mL), dried with anhydrous Na2SO4, filtered, and the filtrate concentrated. The residue was purified by flash chromatography (SiO2, 0.1%-5% MeOH-NH3in CH2Cl2) to afford the title compound as an off-white oil (160 mg, 70%).1H NMR (400 MHz, CDCl3) δ 8.17 – 8.11 (m, 1H), 8.08 – 8.00 (m, 1H), 7.62 – 7.48 (m, 2H), 7.32 – 7.22 (m, 1H), 7.06 (dd, J = 10.4, 7.8 Hz, 1H), 3.29 – 3.18 (m, 2H), 2.69 – 2.61 (m, 2H), 2.39 (s, 6H).13C NMR (101 MHz, CDCl3) δ 157.9 (d, J = 250.1 Hz), 133.1 (d, J = 4.3 Hz), 132.1 (d, J = 4.5 Hz), 127.0, 126.1 (d, J = 8.2 Hz), 125.9 (d, J = 1.9 Hz), 124.2 (d, J = 16.2 Hz), 123.9 (d, J = 2.9 Hz), 121.4 (d, J = 5.8 Hz), 109.1 (d, J = 19.6 Hz), 60.8, 45.5, 31.1. Step 4: 2-(4-fluoronaphthalen-1-yl)-N,N-dimethylethan-1-amine fumarate (I- 76·fumarate) 2-(4-fluoronaphthalen-1-yl)-N,N-dimethylethan-1-amine (120 mg, 0.55 mmol) was formulated as the fumarate salt according to general procedure B and was isolated as white crystals (97 mg, 53%). LCMS (Condition A): tR (4.830 min) m / z = 218.10 [M+H]+;1H NMR (400 MHz, DMSO-d6) δ 8.20 – 8.13 (m, 1H), 8.12 – 8.04 (m, 1H), 7.72 – 7.60 (m, 2H), 7.41 (dd, J = 7.9, 5.6 Hz, 1H), 7.27 (dd, J = 10.7, 7.9 Hz, 1H), 6.57 (s, 2H), 3.34 – 3.37 (m, 2H), 2.95 – 2.88 (m, 2H), 2.55 (s, 6H).13C NMR (151 MHz, DMSO-d6) δ 167.4, 157.0 (d, J = 248.7 Hz), 134.8, 132.5 (d, J = 4.3 Hz), 131.2 (d, J = 4.1 Hz), 127.4, 126.6 (d, J = 8.3 Hz), 126.5, 124.1 (d, J = 2.7 Hz), 123.1 (d, J = 16.1 Hz), 120.5 (d, J = 5.5 Hz), 109.2 (d, J = 19.4 Hz), 58.1, 43.3, 28.1. Example 32: Synthesis of N-ethyl-2-(6-methoxynaphthalen-1-yl)-N-methylethan-1- amine (I-38) Step 1: Methyl 6-methoxy-1-naphthoate (28) To a stirred solution of 6-hydroxy-1-naphthoic acid (10.0 g, 53.1 mmol) in acetone (160 mL) was added dimethyl sulfate (20.1 g, 159.4 mmol) and K2CO3 (27.5 g, 199.3 mmol) at RT. The resulting reaction mixture was stirred at 65 °C for 24 h. TLC indicated completion of the reaction, so the reaction mixture was concentrated under reduced pressure and the residue was dissolved in water (250 mL) and extracted with EtOAc (200 mL x 3). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford the title compound as an orange liquid (10.2 g, 89%).1H NMR (400 MHz, CDCl3): δ 8.85 (d, J = 9.6 Hz, 1H), 8.06 (d, J = 7.2 Hz, 1H), 7.93 (d, J = 8.4 Hz, 1H), 7.48 (t, J = 7.6 Hz, 1H), 7.20 - 7.28 (m, 1H), 7.19 (d, J = 2.4 Hz, 1H), 4.02 (s, 3H), 3.95 (s, 3H). Step 2: (6-methoxynaphthalen-1-yl)methanol (29) To an ice-cold solution of methyl 6-methoxy-1-naphthoate (8.0 g, 37.0 mmol) in THF (80 mL) was added dropwise a suspension of LiAlH4 (2.1 g, 55.5 mmol) in THF (80 mL) under an atmosphere of nitrogen gas. The resulting reaction mixture was stirred at RT for 1 h and then the reaction was cooled again and treated dropwise with 2M HCl (80 mL). TLC indicated completion of the reaction, so the reaction mixture was concentrated under reduced pressure and residue was dissolved in water (80 mL) and extracted with EtOAc (80 mL x 3). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford the title compound as a yellow liquid (5.9 g, 85%).1H NMR (400 MHz, CDCl3): δ 8.07 (d, J = 9.2 Hz, 1H), 7.74 (d, J = 8.4 Hz, 1H), 7.28 - 7.49 (m, 2H), 7.19 - 7.27 (m, 2H), 5.14 (d, J = 5.6 Hz, 2H), 3.96 (s, 3H), 1.71 (t, J = 5.6 Hz, 1H). Step 3: 6-methoxy-1-naphthaldehyde (30) To a stirred solution of (6-methoxynaphthalen-1-yl)methanol (5.9 g, 31.3 mmol) in DCM (80 mL) was added a suspension of pyridinium chlorochromate (13.5 g, 62.7 mmol) in DCM (97 mL) at RT under an atmosphere of nitrogen gas. The resulting reaction mixture was stirred at RT for 1 h and TLC indicated the reaction was complete, so the reaction mixture was diluted with diethyl ether (118 mL). The suspension was filtered through a celite plug and further washed with diethyl ether (50 mL x 3). The combined filtrate was concentrated under reduced pressure to afford the title compound as a brown solid (5.2 g, 89%).1H NMR (400 MHz, CDCl3): δ 10.36 (s, 1H), 9.20 (d, J = 9.2 Hz, 1H), 8.02 (d, J = 8.0 Hz, 1H), 7.86 (d, J = 7.2 Hz, 1H), 7.62 (t, J = 7.6 Hz, 1H), 7.37 (dd, J = 9.2, 2.0 Hz, 1H), 7.24 (s, 1H), 3.97 (s, 3H). Step 4: 6-methoxy-1-(2-methoxyvinyl)naphthalene (31) To an ice-cold solution of potassium tert-butoxide (12.5 g, 111.7 mmol) in anhydrous THF (52 mL) was added 6-methoxy-1-naphthaldehyde (5.2 g, 27.9 mmol) dissolved in anhydrous THF (52 mL) followed by (methoxymethyl)triphenyl phosphonium chloride (23.9 g, 69.8 mmol) under an atmosphere of nitrogen gas. The resulting reaction mixture was stirred at 0 ºC for 1 h at which point the reaction mixture was poured into water (50 mL) and extracted with EtOAc (50 mL x 3). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by flash chromatography (product eluted at 41% EtOAc in hexane) to afford the title compound as an off-white resin (4.2 g, 70%) which was a mixture of E and Z isomers.1H NMR (400 MHz, DMSO-d6): δ 8.03 - 8.10 (m, 1H), 7.80 (d, J = 7.6 Hz, 0.6H), 7.62 - 7.65 (m, 1H), 7.34 - 7.41 (m, 1.4H), 7.28 - 7.30 (m, 1H), 7.13 - 7.17 (m, 1.4H), 6.48 - 6.52 (m, 1H), 5.90 (d, J = 7.2 Hz, 0.6H), 3.87 - 3.88 (m, 3H), 3.75 - 3.77 (m, 3H). Step 5: 2-(6-methoxynaphthalen-1-yl)acetaldehyde (32) To a stirred solution of 6-methoxy-1-(2-methoxyvinyl)naphthalene (1.0 g, 4.66 mmol) in THF (10 mL) was added 5 M aq. HCl (5 mL) at RT and the resulting reaction mixture was stirred at 50 ºC for 1 h. The reaction mixture was then quenched with saturated aq. NaHCO3(20 mL) and extracted with 10% MeOH in DCM (40 mL x 3). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford the title compound as a yellow liquid (0.85 g, 91%).1H NMR (400 MHz, DMSO-d6): δ 9.75 (s, 1H), 7.84 (d, J = 9.2 Hz, 1H), 7.78 (d, J = 8.0 Hz, 1H), 7.43 (t, J = 7.2 Hz, 1H), 7.37 (d, J = 2.0 Hz, 1H), 7.26 (d, J = 6.8 Hz, 1H), 7.19 (dd, J = 9.2, 2.0 Hz, 1H), 4.21 (s, 2H), 3.88 (s, 3H). Step 6: N-ethyl-2-(6-methoxynaphthalen-1-yl)-N-methylethan-1-amine formate (I- 31·formate) To a stirred solution of 2-(6-methoxynaphthalen-1-yl)acetaldehyde (0.8 g, 3.99 mmol) in DCE (16 mL) was added N-methylethanamine (0.47 g, 8.00 mmol) at RT under an atmosphere of nitrogen gas. After 2 h, the reaction was cooled in an ice-bath and NaBH(OAc)3 (2.1 g, 9.98 mmol) was added portion wise. The resulting reaction mixture was stirred at RT for 16 h. The reaction mixture was poured into water (40 mL) and extracted with 10% MeOH in DCM (40 mL x 3). The combined organic layer was dried over Na2SO4 and concentrated under reduced pressure. The residue was purified by reverse phase column chromatography (product eluted at 1% MeCN in water containing 0.05% formic acid) to afford the title compound as the formate salt which was a yellow resin (100 mg, 9%). LCMS (Condition B): tR (1.203 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.22 (s, 1H), 7.96 (d, J = 8.8 Hz, 1H), 7.68 (d, J = 8.0 Hz, 1H), 7.32 - 7.39 (m, 2H), 7.18 - 7.23 (m, 2H), 3.87 (s, 3H), 3.16 (t, J = 7.6 Hz, 2H), 2.67 (t, J = 8.0 Hz, 2H), 2.50 - 2.56 (m, 2H), 2.33 (s, 3H), 1.01 (t, J = 7.2 Hz, 3H). Step 7: N-ethyl-2-(6-methoxynaphthalen-1-yl)-N-methylethan-1-amine fumarate (I- 31·fumarate) N-ethyl-2-(6-methoxynaphthalen-1-yl)-N-methylethan-1-amine formate (100 mg, 0.35 mmol) was reformulated as the fumarate salt according to general procedure B which was isolated as a light-brown solid (70 mg, 56%). LCMS (Condition B): tR (1.236 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.99 (d, J = 9.2 Hz, 1H), 7.69 (d, J = 8.0 Hz, 1H), 7.38 (dd, J = 8.0, 7.2 Hz, 1H), 7.33 (d, J = 2.8 Hz, 1H), 7.18 - 7.25 (m, 2H), 6.55 (s, 2H), 3.87 (s, 3H), 3.19 - 3.23 (m, 2H), 2.78 - 2.83 (m, 2H), 2.66 - 2.70 (m, 2H), 2.45 (s, 3H), 1.06 (t, J = 6.8 Hz, 3H); HPLC purity: 96.6% (270 nm). Example 33: Synthesis of 5-(2-(ethyl(methyl)amino)ethyl)naphthalen-2-ol (I-38) Step 1: 5-(2-(ethyl(methyl)amino)ethyl)naphthalen-2-ol (I-38) To a stirred solution of N-ethyl-2-(2-methoxynaphthalen-1-yl)-N-methylethan-1- amine (700 mg, 2.87 mmol) in CH2Cl2(7 mL) was added 1 M BBr3 in CH2Cl2(3.5 mL) at 0 ºC under an atmosphere of nitrogen gas. The resulting reaction mixture was stirred at RT for 16 h before being poured into saturated aq. NaHCO3(30 mL) and extracted with CH2Cl2(50 mL x 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduce pressure and the crude material was purified by prep-HPLC to afford the title compound as a yellow resin (350 mg, 53%). LCMS (Condition B): tR (1.486 min) m / z = 230.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 9.82 (br. s, 1H), 9.47 (br. s, 1H), 7.95 - 7.98 (m, 1H), 7.62 (d, J = 8.4 Hz, 1H), 7.32 - 7.36 (m, 1H), 7.14 - 7.21 (m, 3H), 3.28 - 3.40 (m, 5H), 3.14 - 3.19 (m, 1H), 2.89 – 2.91 (m, 3H), 1.24 (t, J = 7.2 Hz, 3H). Step 2: 5-(2-(ethyl(methyl)amino)ethyl)naphthalen-2-ol fumarate (I-38·fumarate) 5-(2-(ethyl(methyl)amino)ethyl)naphthalen-2-ol (350 mg, 1.53 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (120 mg, 23%). LCMS (Condition B): tR (1.047 min) m / z = 230.2 [M+H]+;1H NMR (400 MHz, MeOD-d4): δ 7.96 (d, J = 8.8 Hz, 1H), 7.63 (d, J = 8.4 Hz, 1H), 7.34 – 7.39 (m, 1H), 7.26 (d, J = 6.4 Hz, 1H), 7.17 – 7.19 (m, 2H), 6.77 (s, 2H), 3.40 – 3.53 (m, 5H), 3.24 – 3.32 (m, 1H), 3.01 (s, 3H), 1.38 (t, J = 7.2 Hz, 3H); HPLC purity: 100% (210 nm). Example 34: Synthesis of N-(2-(6-methoxynaphthalen-1-yl)ethyl)-N-methylpropan- 2-amine (I-32) Step 1: N-(2-(6-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (I-32) To a stirred solution of 2-(6-methoxynaphthalen-1-yl) acetaldehyde (450 mg, 2.24 mmol) in DCE (9 mL) was added N-methylisopropylamine (490 mg, 6.74 mmol) at RT under an atmosphere of nitrogen gas. After 2 h, NaBH(OAc)3 (1.19 g, 5.61 mmol) was added portion wise at 0 ºC and the resulting reaction mixture was stirred at RT for 16 h. The reaction mixture was then poured into saturated aq. NaHCO3(20 mL) and extracted with 10% MeOH in CH2Cl2(20 mL x 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude material was purified by reverse phase column chromatography (product eluted at 1% MeCN in water containing 0.05% w / w formic acid) to afford the title compound as a yellow liquid (0.15 g, 26%). LCMS (Condition B): tR (1.267 min) m / z = 258.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.94 (d, J = 9.2 Hz, 1H), 7.66 (d, J = 8.0 Hz, 1H), 7.30 - 7.38 (m, 2H), 7.17 - 7.23 (m, 2H), 3.86 (s, 3H), 3.10 (t, J = 7.6 Hz, 2H), 2.87-2.81 (m, 1H), 2.61 (t, J = 7.6 Hz, 2H), 2.26 (s, 3H), 0.92 (d, J = 6.8 Hz, 6H). Step 2: N-(2-(6-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine fumarate (I- 32·fumarate) N-(2-(6-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (150 mg, 0.58 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as a pale-yellow solid (53 mg, 25%). LCMS (Condition B): tR (1.343 min) m / z = 258.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.02 (d, J = 9.2 Hz, 1H), 7.70 (d, J = 8.0 Hz, 1H), 7.36 – 7.41 (m, 1H), 7.33 (d, J = 2.8 Hz, 1H), 7.21 (d, J = 6.4 Hz, 1H), 7.19 (dd, J = 9.2, 2.8 Hz, 1H), 6.56 (s, 2H), 3.87 (s, 3H), 3.27 – 3.31 (m, 3H), 2.92 – 2.97 (m, 2H), 2.54 (s, 3H), 1.09 (d, J = 6.4 Hz, 6H); HPLC purity: 98.8% (210 nm). Example 35: Synthesis of 5-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol (I- 39) Step 1: 5-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol (I-39) To a stirred solution of N-(2-(6-methoxynaphthalen-1-yl)ethyl)-N-methylpropan-2- amine (700 mg, 2.72 mmol) in CH2Cl2(10 mL) was added 1 M BBr3 in CH2Cl2(3.5 mL) at 0 ºC under an atmosphere of nitrogen gas. The resulting reaction mixture was stirred at RT for 2 h before being poured into saturated aq. NaHCO3(100 mL) and extracted with 10% MeOH in CH2Cl2(50 mL x 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by prep-HPLC to afford the title compound as a yellow liquid (500 mg, 76%). LCMS (Condition B): tR (1.091 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 9.81 (br. s, 1H), 9.42 (br. s, 1H), 7.96 - 7.99 (m, 1H), 7.62 (d, J = 8.0 Hz, 1H), 7.34 (t, J = 6.8 Hz, 1H), 7.22 (d, J = 6.8 Hz, 1H), 7.14 - 7.17 (m, 2H), 3.66 - 3.77 (m, 1H), 3.23 - 3.42 (m, 4H), 2.82 – 2.84 (m, 3H), 1.27 (d, J = 6.4 Hz, 3H), 1.21 (d, J = 6.4 Hz, 3H). Step 2: 5-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol fumarate (I-39·fumarate) 5-(2-(isopropyl(methyl)amino)ethyl)naphthalen-2-ol (110 mg, 0.45 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as a white solid (70 mg, 43%). LCMS (Condition B): tR (1.079 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, MeOD-d4): δ 7.96 (d, J = 8.8 Hz, 1H), 7.63 (d, J = 8.4 Hz, 1H), 7.34 – 7.39 (m, 1H), 7.26 (d, J = 7.2 Hz, 1H), 7.17 – 7.19 (m, 2H), 6.77 (s, 2H), 3.73 – 3.80 (m, 1H), 3.42 – 3.55 (m, 3H), 3.33 – 3.39 (m, 1H), 2.95 (s, 3H), 1.40 (d, J = 6.0 Hz, 3H), 1.34 (d, J = 6.4 Hz, 3H); HPLC purity: 100% (210 nm). Example 36: Synthesis of 1-(2-(6-methoxynaphthalen-1-yl)ethyl)azetidine (I-34) Step 1: 1-(2-(6-methoxynaphthalen-1-yl)ethyl)azetidine (I-34) To a stirred solution of 2-(6-methoxynaphthalen-1-yl)acetaldehyde (0.9 g, 4.49 mmol) in DCE (18 mL) was added azetidine (0.76 g, 13.48 mmol) at RT under an atmosphere of nitrogen gas. After 2 h, the reaction was cooled in an ice-bath and NaBH(OAc)3 (2.38 g, 11.23 mmol) was added portion wise. The resulting reaction mixture was stirred at RT for 16 h. The reaction mixture was poured into saturated aq. NaHCO3(50 mL) and extracted with 10% MeOH in DCM (50 mL x 3). The combined organic layer was dried over Na2SO4 and concentrated under reduced pressure. The residue was purified by reverse phase column chromatography (product eluted at 1% MeCN in water containing 0.05% formic acid) to afford the title compound as a yellow resin (80 mg, 7%). LCMS (Condition B): tR (1.226 min) m / z = 242.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.93 (d, J = 9.2 Hz, 1H), 7.66 (d, J = 8.0 Hz, 1H), 7.35 (dd, J = 8.4, 7.2 Hz, 1H), 7.31 (d, J = 2.4 Hz, 1H), 7.17 - 7.20 (m, 2H), 3.86 (s, 3H), 3.10 (t, J = 6.8 Hz, 4H), 2.95 (t, J = 7.2 Hz, 2H), 2.61 (t, J = 7.2 Hz, 2H), 1.93 (p, J = 6.8 Hz, 2H). Step 2: 1-(2-(6-methoxynaphthalen-1-yl)ethyl)azetidine fumarate (I-34·fumarate) 1-(2-(6-methoxynaphthalen-1-yl)ethyl)azetidine (80 mg, 0.33 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as a yellow solid (90 mg, 76%). LCMS (Condition B): tR (1.246 min) m / z = 242.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.99 (d, J = 9.2 Hz, 1H), 7.71 (d, J = 8.4 Hz, 1H), 7.38 (dd, J = 8.0, 7.2 Hz, 1H), 7.33 (d, J = 2.4 Hz, 1H), 7.16 - 7.24 (m, 2H), 6.55 (s, 2H), 3.87 (s, 3H), 3.65 (t, J = 7.6 Hz, 4H), 3.07 - 3.11 (m, 4H), 2.16 (p, J = 7.6 Hz, 2H); HPLC purity: 99.2% (210 nm). Example 37: Synthesis of 5-(2-(azetidin-1-yl)ethyl)naphthalen-2-ol (I-41) Step 1: 5-(2-(azetidin-1-yl)ethyl)naphthalen-2-ol (I-41) To a stirred solution of 1-(2-(6-methoxynaphthalen-1-yl)ethyl)azetidine (450 mg, 1.86 mmol) in CH2Cl2(4.5 mL) was added 1 M BBr3 in CH2Cl2(2.3 mL) at 0 ºC under an atmosphere of nitrogen gas. The resulting reaction mixture was stirred at RT for 2 h before being poured into saturated aq. NaHCO3(30 mL) and extracted with 10% MeOH in CH2Cl2(50 mL x 3). The combined organics were dried over Na2SO4 and concentrated under reduce pressure, and the crude material was purified by prep-HPLC to afford the title compound as a yellow liquid (200 mg, 47%). LCMS (Condition B): tR (1.534 min) m / z = 228.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 9.80 (br. s, 1H), 9.72 (br. s, 1H), 7.92 - 7.95 (m, 1H), 7.62 (d, J = 8.0 Hz, 1H), 7.34 (t, J = 7.2 Hz, 1H), 7.13 - 7.18 (m, 3H), 4.08 - 4.13 (m, 2H), 4.01 - 4.05 (m, 2H), 3.42 - 3.47 (m, 2H), 3.15 – 3.20 (m, 2H), 2.41 - 2.45 (m, 1H), 2.29 - 2.39 (m, 1H). Step 2: 5-(2-(azetidin-1-yl)ethyl)naphthalen-2-ol fumarate (I-41·fumarate) 5-(2-(azetidin-1-yl)ethyl)naphthalen-2-ol (200 mg, 0.88 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (150 mg, 50%). LCMS (Condition B): tR (1.030 min) m / z = 228.2 [M+H]+;1H NMR (400 MHz, MeOD-d4): δ 7.94 (d, J = 8.8 Hz, 1H), 7.63 (d, J = 8.0 Hz, 1H), 7.34 – 7.38 (m, 1H), 7.17 – 7.2 (m, 3H), 6.77 (s, 2H), 4.15 – 4.23 (m, 2H), 4.03 – 4.11 (m, 2H), 3.56 – 3.60 (m, 2H), 3.30 – 3.35 (m, 2H), 2.53 – 2.61 (m, 1H), 2.38 – 2.43 (m, 1H); HPLC purity: 100% (210 nm). Example 38: Synthesis of 1-(2-(6-methoxynaphthalen-1-yl)ethyl)pyrrolidine (I-35) Step 1: 1-(2-(6-methoxynaphthalen-1-yl)ethyl)pyrrolidine (I-35) To a stirred solution of 2-(6-methoxynaphthalen-1-yl)acetaldehyde (1.5 g, 7.5 mmol) in DCE (20 mL) was added pyrrolidine (1.59 g, 22.5 mmol) at RT under an atmosphere of nitrogen gas. After 1 h, the reaction was cooled in an ice-bath and NaBH(OAc)3 (3.9 g, 18.8 mmol) was added portion wise. The resulting reaction mixture was stirred at RT for 16 h. The reaction mixture was poured into saturated aq. NaHCO3(100 mL) and extracted with 10% MeOH in DCM (100 mL x 3). The combined organic layer was dried over Na2SO4 and concentrated under reduced pressure. The residue was purified by reverse phase column chromatography (product eluted at 57% MeCN in water) to afford the title compound as a light-brown liquid (430 mg, 23%). LCMS (Condition B): tR (1.271 min) m / z = 256.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.96 (d, J = 9.6 Hz, 1H), 7.66 (d, J = 8.4 Hz, 1H), 7.36 (dd, J = 8.0, 7.2 Hz, 1H), 7.31 (d, J = 2.4 Hz, 1H), 7.17 - 7.24 (m, 2H), 3.87 (s, 3H), 3.16 (t, J = 7.6 Hz, 2H), 2.65 - 2.70 (m, 2H), 2.49 - 2.52 (m, 4H), 1.66 – 1.72 (m, 4H). Step 2: 1-(2-(6-methoxynaphthalen-1-yl)ethyl)pyrrolidine fumarate (I-35·fumarate) 1-(2-(6-methoxynaphthalen-1-yl)ethyl)pyrrolidine (80 mg, 0.31 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as a yellow solid (90 mg, 77%). LCMS (Condition B): tR (1.262 min) m / z = 256.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 12.11 (br. s, 1H), 8.02 (d, J = 9.2 Hz, 1H), 7.71 (d, J = 8.4 Hz, 1H), 7.37 - 7.41 (m, 1H), 7.34 (d, J = 2.4 Hz, 1H), 7.18 - 7.26 (m, 2H), 6.56 (s, 2H), 3.88 (s, 3H), 3.29 (t, J = 7.6 Hz, 2H), 3.01 (t, J = 7.6 Hz, 2H), 2.90 - 2.96 (m, 4H), 1.80 - 1.86 (m, 4H); HPLC purity: 95.7% (210 nm). Example 39: Synthesis of 5-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol (I-42) Step 1: 5-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol (I-42) To a stirred solution of 1-(2-(6-methoxynaphthalen-1-yl)ethyl)pyrrolidine (350 mg, 1.37 mmol) in CH2Cl2(5 mL) was added 1 M BBr3 in DCM (1.8 mL) at 0 ºC under an atmosphere of nitrogen gas. The resulting reaction mixture was stirred at RT for 2 h before being poured into saturated aq. NaHCO3(100 mL) and extracted with 10% MeOH in CH2Cl2(50 mL x 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduce pressure and the crude material was purified by prep-HPLC to afford the title compound as a yellow liquid (200 mg, 60%). LCMS (Condition B): tR (1.109 min) m / z = 242.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 9.82 (br. s, 1H), 7.95 - 7.98 (m, 1H), 7.62 (d, J = 8.0 Hz, 1H), 7.32 - 7.36 (m, 1H), 7.13 - 7.20 (m, 3H), 3.58 - 3.66 (m, 2H), 3.34 - 3.49 (m, 4H), 3.08 - 3.20 (m, 2H), 1.99 - 2.08 (m, 2H), 1.88 - 1.94 (m, 2H). Step 2: 5-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol fumarate (I-42·fumarate) 5-(2-(pyrrolidin-1-yl)ethyl)naphthalen-2-ol (70 mg, 0.29 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as a pale-yellow solid (80 mg, 77%). LCMS (Condition B): tR (1.090 min) m / z = 242.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 7.96 (d, J = 8.8 Hz, 1H), 7.63 (d, J = 8.4 Hz, 1H), 7.33 - 7.39 (m, 1H), 7.25 (d, J = 2.8 Hz, 1H), 7.17 - 7.19 (m, 2H), 6.77 (s, 2H), 3.70 – 3.82 (m, 2H), 3.44 – 3.59 (m, 4H), 3.12 – 3.26 (m, 2H), 1.98 – 2.22 (m, 4H); HPLC purity: 99.6% (210 nm). Example 40: Synthesis of 2-(6-fluoronaphthalen-1-yl)-N,N-dimethylethan-1-amine (I-44) Step 1: Ethyl 2-(6-fluoro-3,4-dihydronaphthalen-1-yl)acetate (34) NaOEt (2.07 g, 30.5 mmol) was added to anhydrous EtOH (30 mL), followed by triethyl phosphonoacetate (7.25 mL, 36.5 mmol) and the resulting solution was stirred for 10 min. Then, 6-fluoro-1H-tetralone (5 g, 30.5 mmol) was added to the reaction and stirred at reflux under N2 gas for 2.5 h at which point a further portion of NaOEt (1.04 g, 15.3 mmol) and triethyl phosphonoacetate (3.63 mL, 36.5 mmol) in 15 mL of anhydrous EtOH, that had been stirred for 10 min, was added at RT. The reaction was further refluxed under N2 gas for 16 h. Finally, another portion of premixed NaOEt (1.04 g, 15.3 mmol) and triethyl phosphonoacetate (3.63 mL, 36.5 mmol) in 15 mL of anhydrous EtOH, was added at RT and refluxed again under N2 gas for a further 2 h. The reaction mass was then cooled to RT and diluted with H2O (300 mL). The solution was extracted with CH2Cl2(100 mL x 4) and the combined organics washed with saturated aq. NaHCO3(100 mL x 3), then 1 M aq. HCl (100 mL), and then brine (200 mL x 2) before being dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo to afford an orange oil. The residue was purified by flash chromatography (0-5% EtOAc in hexane) to afford the title compound as a mixture of two isomers (ethyl (6-fluoro-1,2,3,4- tetrahydro-1-naphthylidene)acetate : ethyl (6-fluoro-3,4-dihydro-1-naphthyl)acetate; 1:2) as a lightly coloured oil (4.3 g, 60%) which was used in the next step without further purification. Ethyl (6-fluoro-3,4-dihydro-1-naphthyl)acetate:1H NMR (600 MHz, CDCl3): δ 7.17 – 7.10 (m, 1H), 6.92 – 6.79 (m, 2H), 5.95 (t, J = 4.5 Hz, 1H), 4.14 (q, J = 7.1 Hz, 2H), 3.41 (d, J = 1.1 Hz, 2H), 2.82 – 2.73 (m, 2H), 2.31 (dt, J = 12.3, 6.4 Hz, 2H), 1.23 (t, J = 7.1 Hz, 3H);13C NMR (151 MHz, CDCl3): δ 171.9, 161.8 (d, J = 246.3 Hz), 139.1 (d, J = 7.6 Hz), 129.6, 128.3 (d, J = 1.8 Hz), 124.3 (d, J = 8.3 Hz), 114.9 (d, J = 21.5 Hz), 112.8 (d, J = 21.2 Hz), 112.3, 60.9, 39.4, 28.3 (d, J = 1.4 Hz), 23.0, 14.3. Ethyl (6- fluoro-1,2,3,4-tetrahydro-1-naphthylidene)acetate:1H NMR (600 MHz, CDCl3): δ 7.63 (dd, J = 8.8, 5.7 Hz, 1H), 6.92 – 6.79 (m, 2H), 6.25 (t, J = 1.8 Hz, 1H), 4.20 (q, J = 7.1 Hz, 2H), 3.23 – 3.11 (m, 2H), 2.82 – 2.73 (m, 2H), 1.85 (p, J = 6.4 Hz, 2H), 1.31 (t, J = 7.1 Hz, 3H);13C NMR (151 MHz, CDCl3): δ 167.1, 163.5 (d, J = 250.4 Hz), 153.8, 142.9 (d, J = 8.0 Hz), 130.5 (d, J = 3.0 Hz), 127.1 (d, J = 8.6 Hz), 115.5 (d, J = 20.7 Hz), 113.8 (d, J = 21.8 Hz), 112.3, 59.9, 30.4 (d, J = 1.7 Hz), 28.0, 22.6, 14.5. Step 2: Ethyl 2-(6-fluoronaphthalen-1-yl)acetate (35) To a solution of containing a mixture of ethyl (6-fluoro-3,4-dihydro-1- naphthyl)acetate and ethyl (6-fluoro-1,2,3,4-tetrahydro-1-naphthylidene)acetate (3.4 g, 14.5 mmol) in d-limonene (93% purity, 47 mL) was added 10% Pd / C (3.1 g). The resulting suspension was brought to reflux at 180 ºC and within 1 h, an exotherm accompanied by vigorous gas evolution occurred. The reaction was cooled to RT, diluted with EtOAc (200 mL) and filtered through a pad of celite. The residue was washed with EtOAc (3 x 50 mL) and the combined filtrates concentrated in vacuo and the residue was purified by flash chromatography (SiO2, 0-5% EtOAc in hexane) to afford the title compound as a colourless oil (1.16 g, 34%).1H NMR (600 MHz, CDCl3): δ 8.01 (dd, J = 9.2, 5.4 Hz, 1H), 7.73 (d, J = 8.3 Hz, 1H), 7.51 – 7.42 (m, 2H), 7.37 (d, J = 7.0 Hz, 1H), 7.31 (td, J = 8.8, 2.7 Hz, 1H), 4.15 (q, J = 7.1 Hz, 2H), 4.04 (s, 2H), 1.22 (t, J = 7.1 Hz, 3H). Step 3: 2-(6-fluoronaphthalen-1-yl)acetic acid (36) To a stirred mixture of ethyl (6-fluoro-1-naphthyl)acetate (720 mg, 3.10 mmol) in a THF:H2O (1:1, 10 mL) solution was added LiOH (371 mg, 15.5 mmol) in one portion. Stirring was continued for 16 h before being concentrated under a stream of N2 gas. The residue was diluted with H2O (15 mL) and washed with Et2O (2 x 25 mL). The aqueous phase was then adjusted to pH 1-2 by dropwise addition of 6 M aq. HCl and then extracted with CH2Cl2(20 mL x 3). The combined organic layers were washed with brine (50 mL), dried over anhydrous Na2SO4, filtered, and the filtrate was concentrated in vacuo to afford the title compound as a white solid (620 mg, 98%). Step 4: 2-(6-fluoronaphthalen-1-yl)-N,N-dimethylacetamide (37) To a suspension of (6-fluoro-1-naphthyl)acetic acid (500 mg, 2.45 mmol) and EDC.HCl (939 mg, 4.90 mmol) in DMF (5 mL) was added HOBt hydrate (80% w / w, 937 mg, 4.90 mmol), Me2NH.HCl (998 mg, 12.20 mmol), and DIPEA (4.27 mL, 24.50 mmol) at RT. The resulting solution was stirred at RT for 16 h and then diluted with H2O (50 mL) and extracted with EtOAc (20 mL x 5) and the combined organics were washed with saturated aq. Na2CO3 (50 mL x 5) and brine (50 mL x 3) before being dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by column chromatography (SiO2, 0.1%-5% MeOH-NH3in CH2Cl2) to afford the title compound as a colourless oil (415 mg, 73%).1H NMR (400 MHz, CDCl3): δ 8.00 (dd, J = 9.3, 5.5 Hz, 1H), 7.71 (d, J = 8.3 Hz, 1H), 7.51 – 7.38 (m, 2H), 7.36 – 7.26 (m, 2H), 4.13 (s, 2H), 3.04 (s, 6H). Step 5: 2-(6-fluoronaphthalen-1-yl)-N,N-dimethylethan-1-amine hydrochloride (I-44·HCl) To a solution of N,N-dimethyl(6-fluoro-1-naphthyl)acetamide (350 mg, 1.51 mmol) in anhydrous THF (10 mL) was added borane dimethylsulfide complex (2 M in THF, 1.5 mL, 4.32 mmol) under N2 gas and the reaction was warmed to 60 ºC for 1 h. An equal amount of borane dimethylsulfide complex (1.5 mL) was added and stirring was continued at 60 ºC for a further 1 h. The hot solution was then quenched by sequential addition of 6 M aq. HCl (2 mL) then MeOH (3 mL) and stirring continued for a further 15 min. The reaction pH was then adjusted to 11-12 with 5 M aq. NaOH. The suspension was then extracted with EtOAc (100 mL), the organic layer was then washed with saturated aq. Na2CO3 (10 mL x 3) and then 20 mL of a 1:1 solution of brine and saturated aq. Na2CO3. The organic layer was dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by flash chromatography (0 to 20% EtOAc in hexane) to afford the title compound as the borane complex. The complex was dissolved in MeOH (5 mL) and treated with 6 M aq. HCl (1 mL) and stirred at reflux for 1 h. The solvent was removed under a stream of N2 gas and the solid residue was recrystallised from Et2O / i-PrOH to afford the title compound as the hydrochloride salt which was a white solid (150 mg, 41%).1H NMR (400 MHz, DMSO- d6): δ 11.12 (s, 1H), 8.33 (dd, J = 9.3, 5.6 Hz, 1H), 7.85 (d, J = 8.2 Hz, 1H), 7.75 (dd, J = 10.2, 2.7 Hz, 1H), 7.60 – 7.36 (m, 3H), 3.63 – 3.46 (m, 2H), 3.32 – 3.22 (m, 2H), 2.85 (s, 6H);13C NMR (101 MHz, DMSO-d6): δ 159.8 (d, J = 244.1 Hz), 134.5 (d, J = 9.4 Hz), 133.6, 128.4, 127.01 (d, J = 5.0 Hz), 126.96, 126.87, 126.3 (d, J = 2.1 Hz), 116.3 (d, J = 24.9 Hz), 111.6 (d, J = 20.0 Hz), 56.6, 41.9, 27.2; HPLC purity: 99.6% (254 nm). Example 41: Synthesis of N-ethyl-2-(6-fluoronaphthalen-1-yl)-N-methylethan-1- amine (I-45) Step 1: N-ethyl-2-(6-fluoronaphthalen-1-yl)-N-methylacetamide (38) To a suspension of (6-fluoro-1-naphthyl)acetic acid (300 mg, 1.47 mmol) and EDC.HCl (563 mg, 2.94 mmol) in DMF (5 mL) was added HOBt Hydrate (80% w / w, 562 mg, 2.94 mmol) and N-methylethylamine (0.63 mL, 7.35 mmol) at RT. The resulting solution was stirred at RT for 16 h and then diluted with water (50 mL) and extracted with EtOAc (20 mL x 5) and the combined organics were washed with saturated aq. Na2CO3 (50 mL x 5) and brine (50 mL x 3), dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by column chromatography (SiO2, 0.1%-5% MeOH-NH3in CH2Cl2) to afford the title compound as a colourless oil (175 mg, 49%) which was a mixture of rotamers.1H NMR (400 MHz, CDCl3): δ 8.10 – 7.89 (m, 1H), 7.70 (d, J = 8.3 Hz, 1H), 7.51 – 7.37 (m, 2H), 7.33 – 7.24 (m, 2H), 4.21 – 4.05 (m, 2H), 3.58 – 3.27 (m, 2H), 3.06 – 2.92 (m, 3H), 1.22 – 1.00 (m, 3H). Step 2: N-ethyl-2-(6-fluoronaphthalen-1-yl)-N-methylethan-1-amine (I-45) To a solution of N-ethyl-2-(6-fluoronaphthalen-1-yl)-N-methylacetamide (170 mg, 0.69 mmol) in anhydrous THF (5 mL) was added borane dimethylsulfide complex (2 M in THF, 1.4 mL, 2.77 mmol) under N2 gas and the reaction was stirred at reflux for 1 h. Upon completion, the hot solution was quenched by sequential addition 6 M aq. HCl (3 mL) followed by MeOH (5 mL). The solution was then stirred at reflux for 1 h, and then concentrated under a stream of N2 gas. The aqueous residue was neutralised with saturated aq. Na2CO3 and then made a basic with 15% aq. NaOH (1 mL). The suspension was extracted with CH2Cl2(20 mL x 3), and the organics washed with saturated aq. Na2CO3 (10 mL x 3), brine (20 mL), before being dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by flash chromatography (SiO2, 0.1%-2% MeOH-NH3in CH2Cl2) to afford the title compound as a colourless oil (119 mg, 48%).1H NMR (400 MHz, CDCl3): δ 8.06 (dd, J = 9.3, 5.5 Hz, 1H), 7.65 (d, J = 8.2 Hz, 1H), 7.50 – 7.38 (m, 2H), 7.34 – 7.26 (m, 2H), 3.34 – 3.20 (m, 2H), 2.81 – 2.67 (m, 2H), 2.58 (q, J = 7.2 Hz, 2H), 2.41 (s, 3H), 1.13 (t, J = 7.2 Hz, 3H);13C NMR (101 MHz, CDCl3): δ 160.5 (d, J = 245.8 Hz), 137.0, 135.0 (d, J = 9.1 Hz), 129.2 (d, J = 0.8 Hz), 126.9, 126.42 (d, J = 8.1 Hz), 126.35 (d, J = 3.7 Hz), 125.9 (d, J = 2.4 Hz), 116.3 (d, J = 25.0 Hz), 111.8 (d, J = 19.9 Hz), 58.5, 51.5, 41.7, 31.3, 12.4. Step 3: N-ethyl-2-(6-fluoronaphthalen-1-yl)-N-methylethan-1-amine fumarate (I- 45·fumarate) N-ethyl-2-(6-fluoronaphthalen-1-yl)-N-methylethan-1-amine (80 mg, 0.35 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as white crystals (75 mg, 60%).1H NMR (400 MHz, DMSO-d6): δ 8.21 (dd, J = 9.3, 5.7 Hz, 1H), 7.81 (d, J = 8.2 Hz, 1H), 7.73 (dd, J = 10.2, 2.7 Hz, 1H), 7.54 – 7.38 (m, 3H), 6.57 (s, 2.2H), 3.41 - 3.30 (m, 2H), 3.03 – 2.96 (m, 2H), 2.87 (q, J = 7.2 Hz, 2H), 2.59 (s, 3H), 1.13 (t, J = 7.2 Hz, 3H);13C NMR (101 MHz, DMSO-d6): δ 167.1, 159.8 (d, J = 243.7 Hz), 135.3, 134.7, 134.5 (d, J = 9.3 Hz), 128.6, 127.0, 126.8 (d, J = 9.0 Hz), 126.6 (d, J = 5.2 Hz), 126.2 (d, J = 2.0 Hz), 116.2 (d, J = 24.9 Hz), 111.5 (d, J = 20.0 Hz), 56.0, 50.1, 39.4, 28.3, 10.3. HPLC purity: 98.3% (254 nm). Example 42: Synthesis of N-(2-(6-fluoronaphthalen-1-yl)ethyl)-N-methylpropan-2- amine (I-46) Step 1: 2-(6-fluoronaphthalen-1-yl)-N-isopropyl-N-methylacetamide (39) To a suspension of (6-fluoro-1-naphthyl)acetic acid (300 mg, 1.47 mmol) and EDC.HCl (563 mg, 2.94 mmol) in DMF (5 mL) was added HOBt Hydrate (80% w / w, 562 mg, 2.94 mmol) and N-methyl(isopropyl)amine (0.77 mL, 7.35 mmol) at RT. The resulting solution was stirred at RT for 16 h and then diluted with H2O (50 mL) and extracted with EtOAc (20 mL x 5) and the combined organics were then washed sequentially with saturated aq. Na2CO3 (50 mL x 5), followed by brine (50 mL x 3) before being dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by column chromatography (SiO2, 0.1%-5% MeOH- NH3in CH2Cl2) to afford the title compound as a colourless oil (375 mg, 98%) which was a mixture of rotamers (approximately 1:2, A:B).1H NMR (400 MHz, CDCl3): δ 8.08 – 7.90 (m, 1H), 7.70 (d, J = 8.3 Hz, 1H), 7.52 – 7.39 (m, 2H), 7.36 – 7.26 (m, 2H), 5.06 – 4.84 (m, 0.6H; rotamer B), 4.24 – 4.06 (m, 2.4H), 2.92 – 2.78 (m, 3H), 1.20 – 1.05 (m, 6H). Step 2: N-(2-(6-fluoronaphthalen-1-yl)ethyl)-N-methylpropan-2-amine (I-46) To a solution of 2-(6-fluoronaphthalen-1-yl)-N-isopropyl-N-methylacetamide (370 mg, 1.43 mmol) in anhydrous THF (10 mL) was added borane dimethylsulfide complex (2 M in THF, 2.85 mL, 5.71 mmol) under N2 gas and the reaction was stirred at reflux for 1 h. Upon completion, the hot solution was quenched by sequential addition of 6 M aq. HCl (2 mL), followed by MeOH (5 mL). The solution was then stirred at reflux for 1 h, and then concentrated under a stream of N2 gas. The aqueous residue was neutralised with saturated aq. Na2CO3 and then made a basic with 1 mL of 15% aq. NaOH. The suspension was extracted with CH2Cl2(50 mL x 3), and the combined organics washed with saturated aq. Na2CO3 (20 mL x 3) and brine (50 mL). The organic layer was dried over anhydrous Na2SO4, filtered, and the filtrate concentrated in vacuo. The residue was purified by flash chromatography (SiO2, 0.1%-2% MeOH-NH3in CH2Cl2) to afford the title compound as a colourless oil (305 mg, 87%).1H NMR (400 MHz, CDCl3): δ 8.07 (dd, J = 9.3, 5.5 Hz, 1H), 7.65 (d, J = 8.2 Hz, 1H), 7.50 – 7.37 (m, 2H), 7.35 – 7.26 (m, 2H), 3.28 – 3.18 (m, 2H), 2.96 (sept, J = 6.5 Hz, 1H), 2.82 – 2.65 (m, 2H), 2.41 (s, 3H), 1.05 (d, J = 6.6 Hz, 6H);13C NMR (101 MHz, CDCl3): δ 160.5 (d, J = 246.0 Hz), 137.3, 135.0 (d, J = 8.9 Hz), 129.2, 126.9, 126.5 (d, J = 8.9 Hz), 126.3 (d, J = 5.1 Hz), 125.9 (d, J = 2.2 Hz), 116.2 (d, J = 24.9 Hz), 111.8 (d, J = 19.8 Hz), 54.8, 53.9, 37.4, 32.4, 18.1. Step 3: N-(2-(6-fluoronaphthalen-1-yl)ethyl)-N-methylpropan-2-amine fumarate (I- 46·fumarate) Fumaric acid (142 mg, 1.22 mmol) was dissolved in minimal refluxing acetone and then treated with a solution of N-(2-(6-fluoronaphthalen-1-yl)ethyl)-N-methylpropan- 2-amine (300 mg, 1.22 mmol) dissolved in minimal acetone before being concentrated under a stream of N2gas to produce an oil. The oil was then triturated with Et2O and the resulting solid was collected by vacuum filtration, washed with Et2O and air dried to afford the title compound as the fumarate salt which was a white solid (400 mg, 91%).1H NMR (400 MHz, DMSO-d6): δ 8.23 (dd, J = 9.3, 5.6 Hz, 1H), 7.81 (d, J = 8.1 Hz, 1H), 7.72 (dd, J = 10.2, 2.7 Hz, 1H), 7.60 – 7.34 (m, 3H), 6.57 (s, 2H), 3.43 – 3.28 (m, 3H), 3.08 – 2.90 (m, 2H), 2.58 (s, 3H), 1.13 (d, J = 6.6 Hz, 6H);13C NMR (101 MHz, DMSO- d6): δ 167.6, 159.8 (d, J = 243.8 Hz), 135.2, 134.9, 134.5 (d, J = 9.2 Hz), 128.6, 127.0, 126.8 (d, J = 9.0 Hz), 126.6 (d, J = 5.0 Hz), 126.3 (d, J = 2.1 Hz), 116.2 (d, J = 24.8 Hz), 111.5 (d, J = 20.0 Hz), 54.4, 53.1, 34.8, 28.7, 16.5. HPLC purity: 98.3% (254 nm). Example 43: Synthesis of 1-(2-(6-fluoronaphthalen-1-yl)ethyl)azetidine (I-49) Step 1: 2-(6-fluoronaphthalen-1-yl)ethan-1-ol (40) To a stirred solution of ethyl 2-(6-fluoronaphthalen-1-yl)acetate (1.0 g, 4.31 mmol) in THF (10 mL) was added LiAlH4 (0.24 g, 6.46 mmol) at 0 ºC. The reaction mixture was stirred at 0 °C to RT for 2 h. The reaction mixture was poured into water (200 mL) and extracted EtOAc (200 mL x 3). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford the title compound as a pale-yellow liquid (1.2 g) which was used in the next step without further purification.1H NMR (400 MHz, DMSO-d6): δ 8.14 (dd, J = 9.2, 5.6 Hz, 1H), 7.76 (d, J = 8.4 Hz, 1H), 7.69 (dd, J = 10.4, 2.8 Hz, 1H), 7.41 - 7.48 (m, 2H), 7.36 (d, J = 6.8 Hz, 1H), 4.75 (t, J = 5.2 Hz, 1H), 3.68 – 3.73 (m, 2H), 3.18 - 3.21 (m, 2H). Step 2: 2-(6-fluoronaphthalen-1-yl)ethyl methanesulfonate (41) To a stirred solution of 2-(6-fluoronaphthalen-1-yl)ethan-1-ol (1.2 g, 6.31 mmol) in DCM (18 mL) were added TEA (2.5 mL, 18.9 mmol) and MsCl (1.5 mL, 9.47 mmol) at 0 °C and reaction mixture was stirred at RT for 2 h. The reaction mixture was quenched with water (100 mL) and extracted with EtOAc (100 mL x 2). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduced pressure to afford the title compound as a pale-yellow liquid (1.5 g, 89%).1H NMR (400 MHz, DMSO-d6): δ 8.20 (dd, J = 9.6, 5.6 Hz, 1H), 7.84 (d, J = 8.4 Hz, 1H), 7.74 (dd, J = 10.0, 2.8 Hz, 1H), 7.43 - 7.53 (m, 3H), 4.50 (t, J = 6.8 Hz, 2H), 3.49 (t, J = 6.8 Hz, 2H), 3.10 (s, 3H). Step 3: 1-(2-(6-fluoronaphthalen-1-yl)ethyl)azetidine (I-49) To a stirred solution of 2-(6-fluoronaphthalen-1-yl)ethyl methanesulfonate (500 mg, 1.86 mmol) in MeCN (5 mL) was added K2CO3 (1.2 g, 9.32 mmol) and azetidine (130 mg, 2.23 mmol) at RT and the reaction mixture was then stirred at 80 ºC for 16 h. The reaction mixture was then poured into water (70 mL) and extracted with EtOAc (70 mL x 2). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduce pressure and the crude material was purified by reverse phase column chromatography (product eluted at 49% MeCN in water) to afford the title compound as a pale-yellow sticky solid (0.18 g, 42%). LCMS (Condition B): tR (1.624 min) m / z = 230.1 [M+H]+; HPLC purity: 99.34% (210 nm);1H NMR (400 MHz, DMSO-d6): δ 8.11 (dd, J = 9.2, 5.6 Hz, 1H), 7.77 (d, J = 8.0 Hz, 1H), 7.70 (dd, J = 10.0, 2.4 Hz, 1H), 7.42 - 7.48 (m, 2H), 7.34 (d, J = 6.8 Hz, 1H), 3.11 (t, J = 6.8 Hz, 4H), 3.00 (t, J = 7.6 Hz, 2H), 2.64 (t, J = 7.6 Hz, 2H), 1.90 - 1.97 (m, 2H). Step 4: 1-(2-(6-fluoronaphthalen-1-yl)ethyl)azetidine fumarate (I-49·fumarate) 1-(2-(6-fluoronaphthalen-1-yl)ethyl)azetidine (180 mg, 0.78 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (225 mg, 83%). LCMS (Condition B): tR (1.641 min) m / z = 230.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.17 (dd, J = 9.2, 5.6 Hz, 1H), 7.81 (d, J = 8.0 Hz, 1H), 7.73 (dd, J = 10.0, 2.8 Hz, 1H), 7.44 – 7.51 (m, 2H), 7.38 (d, J = 6.4 Hz, 1H), 6.56 (s, 2H), 3.57 (t, J = 7.6 Hz, 4H), 3.12 – 3.17 (m, 2H), 2.99 – 3.04 (m, 2H), 2.10 – 2.18 (m, 2H); HPLC purity: 97.2% (210 nm). Example 44: Synthesis of 1-(2-(6-fluoronaphthalen-1-yl)ethyl)pyrrolidine (I-50) Step 1: 1-(2-(6-fluoronaphthalen-1-yl)ethyl)pyrrolidine (I-50) To a stirred solution of 2-(6-fluoronaphthalen-1-yl)ethyl methanesulfonate (500 mg, 1.86 mmol) in MeCN (5 mL) was added K2CO3 (1.2 g, 9.32 mmol) and pyrrolidine (150 mg, 2.24 mmol) at RT and the reaction mixture was stirred at 80 ºC for 16 h. The reaction mixture was poured into water (100 mL) and extracted with EtOAc (60 mL x 2). The combined organics were dried over anhydrous Na2SO4 and concentrated under reduced pressure, and the crude material was purified by reverse phase column chromatography (product eluted at 49% MeCN in water) to afford the title compound as an off-white resin (220 mg, 49%). LCMS (Condition B): tR (1.218 min) m / z = 244.1 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.13 (dd, J = 9.2, 5.6 Hz, 1H), 7.76 (d, J = 8.0 Hz, 1H), 7.69 (dd, J = 10.4, 2.8 Hz, 1H), 7.42 - 7.47 (m, 2H), 7.37 (d, J = 6.4 Hz, 1H), 3.18 – 3.23 (m, 2H), 2.67 - 2.71 (m, 2H), 2.49 - 2.53 (m, 4H), 1.67 - 1.70 (m, 4H). Step 2: 1-(2-(6-fluoronaphthalen-1-yl)ethyl)pyrrolidine fumarate (I-50·fumarate) 1-(2-(6-fluoronaphthalen-1-yl)ethyl)pyrrolidine (220 mg, 0.90 mmol) was formulated as the fumarate salt according to general procedure B which was isolated as an off-white solid (250 mg, 78%). LCMS (Condition B): tR (1.236 min) m / z = 244.2 [M+H]+;1H NMR (400 MHz, DMSO-d6): δ 8.22 (dd, J = 9.2, 5.6 Hz, 1H), 7.81 (d, J = 8.0 Hz, 1H), 7.72 (dd, J = 10.0, 2.4 Hz, 1H), 7.40 – 7.51 (m, 3H), 6.56 (s, 2H), 3.36 – 3.40 (m, 2H), 3.10 – 3.13 (m, 2H), 3.04 – 3.09 (m, 4H), 1.83 – 1.89 (m, 4H); HPLC purity: 95.9% (210 nm). Table 2 Agonist activity of exemplified compounds at selected serotonin (5-HT) receptors in Ca2+flux functional assays. Notes: cells absent data indicate that the compound was not tested at the time of filing. These data may be obtained by analogous methods to those described herein. Receptor Profiling: Activity at 5-HT2A, 5-HT1A, 5-HT2B and 5-HT2C receptors was determined using a FLIPR Ca2+ flux assay at WuXi AppTec Co. Ltd. (Hong Kong) Discovery Biology Unit according to their standard protocols. Briefly, stably transfected cells expressing the receptor of interest (HEK293 for 5-HT2A and 5-HT2C; CHO-K1 for 5- HT2B) were grown and plated in a 384 well plate and incubated at 37 °C and 5% CO2 overnight. A 250 mM stock solution of probenecid in FLIPR calcium assay buffer (10 mL) was freshly prepared and combined with a fluorescent dye (Fluo-4 Direct) to give a final assay concentration of 2.5 mM. Reference compounds were 4-fold serially diluted and the screening compounds were 3-fold serially diluted in 100% DMSO for 10 points using Agilent Bravo, and 750 nL was added to a 384 well compound plate using Echo along with 30 µL assay buffer. The fluorescent dye was then added to the assay plate along with assay buffer to a final volume of 40 µL. The cell plate was incubated for 50 min at 37 °C and 5% CO2and placed into the FLIPR Tetra along with the compound plate.10µL of references and compounds were then transferred from the compound plate into the cell plate and the fluorescent signal was read. In vivo pharmacokinetics experiments Prospective studies for in vivo pharmacokinetics will be conducted using established procedures in accordance with the Australian Code of Practice for the Care and Use of Animals for Scientific Purposes, and the study protocols will be reviewed and approved by the Monash Institute of Pharmaceutical Sciences Animal Ethics Committee. A brief outline of a standard, previously used method is described below: The systemic exposure of selected examples will be studied in non-fasted male C57BL / 6 mice weighing between 18.9 – 25.5 g. Mice will have access to food and water ad libitum throughout the pre- and post-dose sampling period. On the day of dosing, the formulation of each compound will be prepared by dissolving solid compound in an appropriate solvent using vortexing. Compounds will be dosed to mice by IP injection (10 mL / kg dose volume via a 27G needle; n=9 mice per compound) and blood samples will be collected at various time points (e.g.5 and 30 min; 1, 2 and 4 h post-dose (n=3 mice per time point for each compound)). A maximum of three blood samples will be obtained from each mouse, with plasma samples being taken via submandibular bleed (approximately 120 μL). Once collected, blood samples will be processed by standard methods and analysed by LCMS. In addition, whole brain samples will be taken by rapid removal from the carcass soon after the blood collection. The whole brains will be blotted to remove excess blood, placed into pre-weighed polypropylene vials, and weighed. The brains will be snap frozen in dry ice and subsequently stored frozen (-80 °C) until analysis. Bioanalytical Method Summary: Concentrations of test compound in plasma and tissue samples will be determined using an LCMS / MS method validated for linearity, accuracy, precision, matrix factor and recovery. Test compound standard solutions will be diluted from a concentrated stock solution (32 mM in H2O) using 50% ACN in H2O (v / v) and a calibration curve was prepared in a matched matrix to the test samples. Plasma: The plasma calibration curve will be prepared by spiking aliquots of blank mouse plasma (25 μL) with test compound standard solutions (5 μL) and internal standard solution (5 μL of diazepam, 5 μg / mL in 50% acetonitrile in water). Test plasma samples (25 μL) will be thawed, mixed, and then spiked with internal standard solution (5 μL). Plasma protein precipitation can be performed by addition of acetonitrile (3-fold volume ratio) and thorough vortex mixing. Samples will be centrifuged (RCF = 9391 x g) for 3 minutes and the supernatant (90 μL) collected for analysis. Tissue: Pre-weighed tissue samples (brain) will be prepared according to general methods, for example: homogenised using a glass rod in buffer containing an EDTA / potassium fluoride solution (0.1 M / 4 mg / mL) as a stabilisation cocktail to minimise the potential for ex vivo degradation (3 mL cocktail / g tissue). The tissue homogenate will be briefly centrifuged (RCF = 79 x g) for 10 seconds to separate the foam layer before transferring an aliquot of the tissue homogenate (200 μL) to a fresh Eppendorf tube for sample extraction. Calibration standards will be prepared by spiking blank brain homogenate (200 μL) with the solution standards (10 μL) and the internal standard (10 μL). Study samples can be similarly prepared, except that acetonitrile (10 μL) was added instead of solution standards to maintain the same volume. Protein precipitation can be carried out by the addition of a 3-fold volume of acetonitrile, followed by vortex mixing and centrifugation (RCF = 9391 x g) for 3 min to recover the supernatant for analysis. Replicate analysis: Triplicate analytical replicate (ARs) samples will be prepared similarly to the standards for each sample type at three concentrations (50, 500 and 2,000 ng / mL) and repeat injections of these ARs will be included throughout the analytical run to assess assay performance. The extraction of the test compound from the standards and ARs will be conducted as described above. All test samples will be quantified within the calibration range of the assay and the stability of each test compound will be confirmed in homogenate during the period of sample processing (15 min; < 15% loss). Biotelemetry and Head-Twitch Response (HTR) experiments Psychedelic potential will be assessed via the industry standard head twitch response in Mice (C57BL / 6J males). The study will be conducted through standard means of which are summarised below. Mice will be purchased from the Jackson Laboratory (Bar Harbor, ME, USA) at 5−6 weeks of age and allowed at least 1−2 weeks to acclimate to the animal research facility. Mice will be initially group housed 3−5 per cage during acclimation and housed in a 12 h light−dark cycle throughout the study, with lights on at 0700 h. Food and water will be available ad libitum except during testing. Cohorts of 20−24 mice will be used for each test drug. The mice will be subjected to experimental testing once every 1−2 weeks for 2−3 months to complete dose−effect curves and antagonist experiments. A minimum of 7 days between treatments will be utilized to avoid any tolerance to effects of repeated drug administration. All drug doses represent the weight of the salt dissolved in 0.9% saline vehicle. Mice will be tested first in dose−response studies to assess the effects of each compound at doses from 0.03 to 30 mg / kg s.c. and will be subsequently tested in antagonist reversal studies utilizing pretreatment with M100907 and WAY100635. All experiments will be conducted from 0900 to 1700 local time during the light phase, as sensitivity of rodents to other tryptamine psychedelics is diurnal, with maximal HTR observed in the middle of the light phase. Experiments will be run during the light phase also to avoid any potential influence of melatonin receptor activity on HTR as melatonin and related agonists are known to reduce HTR induced by DOI in rats. For each experiment, mice will be acclimated to the testing room in their home cage for at least 1 h prior to experimental sessions. Behavioral test sessions will be carried out in Tru Scan mouse locomotor arenas equipped with photobeam arrays (Coulbourn Instruments, Holliston, MA, USA), which will be modified with cylindrical inserts and transparent floors useful in detecting mouse HTR. Subcutaneous Temperature Transponder Implants. At least 1 week prior to the start of the experiments, mice will recieve s.c. implanted temperature transponders (14 × 2 mm, model IPTT-300, Bio Medic Data Systems, Inc., Seaford, DE, USA) under brief isoflurane anesthesia. Mice were single housed post implant for the remainder of the study to protect the transponder from removal by cage mates. Temperature will be determined noninvasively using a handheld receiver that is sensitive to signals emitted from the implanted transponders. Prior to each experiment, mouse body weight and temperature will be recorded. Mice will then be placed into testing chambers for acclimation. In dose−response studies, after a brief 5 min acclimation, mouse body temperature will be recorded for baseline measurement, mice will receive s.c. injection of test substance or vehicle, and animals will be returned to the testing arena for 30 min. During the session, locomotor activity will be monitored via photobeam tracking of movements in the horizontal plane to yield distance traveled in centimeter. HTR will be monitored by the analysis of GoPro Hero Black 7 video recordings (120 frames per sec and 960p resolution) using a commercially available software package from Clever Sys Inc. (Reston, VA, USA).82 post-treatment body temperature values will also be recorded, and temperature data is represented as change from pretreatment baseline. In antagonist reversal experiments, mice will recieve a s.c. injection of either receptor antagonists or vehicle and were returned to the testing chamber for 30 min. During this period, locomotor activity will be monitored to examine the potential effects of antagonist treatment on general behavior or movement. At 30 min after antagonist administration, mice will be given test drug or vehicle and returned to the chambers for an additional 30 min of video recording used for analyses. All statistical analyses will be conducted using GraphPad Prism 9 (La Jolla, CA, USA). Dose−response data from mouse experiments will be analyzed using nonlinear regression, and potency values will be determined from the rising phase of the curves for HTR measures. For mouse studies, one-way ANOVA with Dunnett’s post hoc test will be used to compare all conditions to vehicle controls (0 or 0,0) in dose−response and antagonist experiments. Mean HTR count, distance traveled, and temperature change for each condition will be used for statistical comparisons. Alpha will be set at 0.05 for all analyses. Acute Restraint Stressor (ASR) Tail Suspension Test (TST) in mice Compounds will be assessed in a validated model of depression conducted the leading contract research organisation; Europhins Panlabs. The assessment will be conducted according to standard conditions and are briefly outlined Here: Male ICR mice (23 ± 3 g) will be purchased from BioLASCO (Taipei, Taiwan) at 4-5 weeks of age and allowed 5-7 days to acclimate to the animal research facility at Pharmacology Discovery Services (Taipei, Taiwan). Mice will be housed in groups of 10 in a large cage (47 x 25 x 15 cm) on a 12-hour light cycle (lights on: 0700) and provided ad libitum food and water except during acute restraint stress and tail-suspension testing. Temperature will be maintained at 20-24 °C, and all rooms (colony and testing rooms) had similar lighting intensity. All aspects of this work including housing, experimentation, and animal disposal were performed in accordance with the “Guide for the Care and Use of Laboratory Animals: Eighth Edition” (The National Academies Press, Washington, DC, 2011) in a facility accredited by the Association for Assessment and Accreditation of Laboratory Animal Care. All experiments will be conducted between 0900 to 1700 local time, during the light phase. Each mouse will undergo a single behavioural experiment in which they were randomly allocated to receive a single treatment with vehicle (50mM phosphate buffered saline, pH = 6.5), Ketamine as a positive control (10 mg / kg, diluted in 0.9% saline from 50 mg / ml stock), or one dose of a test drug (n=10 per dose of test drug, n=12 for vehicle, n=12 for ketamine). All drug doses represent the freebase dose in salt form dissolved in vehicle. All solutions will be delivered at 5 ml / kg via intraperitoneal injection. Acute Restraint Stress (ARS) Procedure: Mice will be moved from the colony room to the procedure room in which ARS will be performed. Mice will recieve oral gavage of water (10 ml / kg) to avoid dehydration, and then will be individually restrained for 5 hours in a clear plastic cylinder (50 mL centrifuge tube with air holes drilled for ventilation), positioned horizontally on a bench with bench towel to absorb urine. This restraint will prevent physical movement, without causing pain. Restrainers will be washed with veterinary disinfectant between mice. Drug Administration: Immediately after the 5-hour ARS procedure, mice will be removed from the restrainers, placed in their home cage, and transported to the room in which Tail Suspension Test will be be conducted. Mice will then receive intraperitoneal injection with vehicle, ketamine (10 mg / kg), test compounds (over a range of doses), and will be placed back in their home cage.10 minutes after treatment, animals will undergo the Tail Suspension Test. Tail Suspension Test (TST) Procedure: Mice will be individually suspended on the edge of a shelf, 58 cm above a tabletop, using adhesive tape placed approximately 1 cm from the tip of the tail, for a total duration of 7 minutes. Using a stopwatch, the experimenters blinded to treatment groups will record the duration of immobility (defined as hanging passively and motionless) during the 5 minutes spanning from 2-7 minutes. The data from 0-2 minutes will not be recorded. Mice undergoing TST will never be in view of other mice. Following TST, mice will be euthanized via carbon dioxide inhalation. Statistical Analysis: Statistical analyses will be conducted using GraphPad Prism 9 (La Jolla, CA, USA), using a priori simple effect comparisons within a one-way ANOVA to compare the test compounds to the Vehicle condition, on time spent immobile (in seconds). STATEMENTS 1. A compound of formula (I): or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein L is selected from C1-4 alkylene, C2-4 alkenylene and C2-4 alkynylene; R1is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4- C14 alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8 alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R2is independently selected from hydrogen, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; alternatively R1and R2together with the atoms to which they are attached form a C3-8heterocycloalkyl including 0, 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR11, said C3-8heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-8alkylamino, C1-8alkylsulfonyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R3is selected from hydrogen, C1-6alkyl, C3-8cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R3and one of R1and R2together with the atoms to which they are attached form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; each R11is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl, and C3-7heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl and C3-7heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R12, C(O)N(R12)2, OR12, N(R12)2, NO2, SR12and SO2R12, said C3-C7cycloalkyl and C3-7heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12; each R12is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8 alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, CN, OR13, N(R13)2, SR13, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, C4-16alkyleneheteroaryl; said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13and SO2R13, said C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein at least one of R4, R5, R6and R8is other than hydrogen. 2. The compound of statement 1, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein the compound is not pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, or polymorph thereof. 3. The compound of statement 1 or 2, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein the compound is not pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, or polymorph thereof. 4. The compound of any one of the preceding statements, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein the compound is not pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, or polymorph thereof. 5. The compound of any one of the preceding statements, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein the compound is not or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, or polymorph thereof. 6. The compound of any one of the preceding statements, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein the compound is not pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, or polymorph thereof. 7. The compound of any one of the preceding statements, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein the compound is not or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, or polymorph thereof. 8. The compound of any one of the preceding statements, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein the compound is not or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, or polymorph thereof. 9. The compound of any one of the preceding statements, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein the compound is not pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, or polymorph thereof. 10. The compound of any one of the preceding statements, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorp...

Claims

CLAIMS 1. A compound of formula (I):or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein L is selected from C1-4 alkylene, C2-4 alkenylene and C2-4 alkynylene; R1is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4- C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R2is independently selected from hydrogen, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; alternatively R1and R2together with the atoms to which they are attached form a C3-8heterocycloalkyl including 0, 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR11, said C3-8heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-8alkylamino, C1-8alkylsulfonyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R3is selected from hydrogen, C1-6alkyl, C3-8cycloalkyl, or C4-14 alkylenecycloalkyl;alternatively R3and one of R1and R2together with the atoms to which they are attached form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; each R11is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl, and C3-7heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl and C3-7heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R12, C(O)N(R12)2, OR12, N(R12)2, NO2, SR12and SO2R12, said C3-C7cycloalkyl and C3-7heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12; each R12is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, CN, OR13, N(R13)2, SR13, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, C4-16alkyleneheteroaryl; said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13and SO2R13, said C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein i) the compound is not selected from the group consisting of: , , ,, , , or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, or polymorph thereof; andii) wherein at least one of R4, R5, R6and R8is other than hydrogen.

2. The compound of claim 1, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, OR13, C1-2 alkyl, C1-2 haloalkyl, C1-2 alkoxy and C1-2 haloalkoxy; and R13is independently selected from hydrogen, C1-2 alkyl, and C1-2 haloalkyl.

3. The compound of claim 1 or 2, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, OR13, C1-2 alkyl; R13is independently selected from hydrogen and C1-2 alkyl.

4. The compound of any one of claims 1 to 3, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, fluoro, and OR13; and R13is hydrogen.

5. The compound of any one of claims 1 to 4, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein one of R4, R5, R6and R8is other than hydrogen.

6. The compound of any one of claims 1 to 5, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein R4is other than hydrogen.

7. The compound of any one of claims 1 to 5, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein R5is other than hydrogen.

8. The compound of any one of claims 1 to 5, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein R6is other than hydrogen.

9. The compound of any one of claims 1 to 5, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein R8is other than hydrogen.

10. The compound of any one of claims 1 to 9, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph and / or prodrug thereof, wherein R1and R2are each independently selected from hydrogen, C1-4 alkyl, C1-4 haloalkyl, C3-4 cycloalkyl, C4-5 alkylenecycloalkyl, and C7alkylenearyl; or wherein R1and R2together with the atoms to which they are attached form a C3-6heterocycloalkyl including 0, 1 or 2 additional ring heteromoieties selected from O, N and NR11.

11. The compound of any one of claims 1 to 10, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R1and R2, together with the nitrogen to which they are attached, form any one of the following:, , , , , ,12. The compound of any one of claims 1 to 11, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R3is hydrogen.

13. The compound of any one of claims 1 to 12, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein L is methylene.

14. The compound of any one of claims 1 and 10 to 13, or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, wherein R6is selected from OH and F, and R4, R5, R7, R8, R9and R10are each H.

15. The compound of claim 1, selected from:or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof.

16. A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof; and a pharmaceutically acceptable excipient;wherein L is selected from C1-4 alkylene, C2-4 alkenylene and C2-4 alkynylene; R1is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4- C14 alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R2is independently selected from hydrogen, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11,said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; alternatively R1and R2together with the atoms to which they are attached form a C3-8heterocycloalkyl including 0, 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR11, said C3-8heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-8alkylamino, C1-8alkylsulfonyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R3is selected from hydrogen, C1-6alkyl, C3-8cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R3and one of R1and R2together with the atoms to which they are attached form a C3-12heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; each R11is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl, and C3-7heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12,said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl and C3-7heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R12, C(O)N(R12)2, OR12, N(R12)2, NO2, SR12and SO2R12, said C3-C7cycloalkyl and C3-7heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12; each R12is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, CN, OR13, N(R13)2, SR13, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, C4-16alkyleneheteroaryl;said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13and SO2R13, said C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein at least one of R4, R5, R6and R8is other than hydrogen.

17. A pharmaceutical composition comprising a compound of any one of claims 1 to 15 or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, and a pharmaceutically acceptable excipient.

18. A method of treating a disease, disorder or condition by activation of a serotonin receptor, the method comprising administering to a subject in need thereof a compound of formula (I):wherein L is selected from C1-4 alkylene, C2-4 alkenylene and C2-4 alkynylene; R1is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4- C14 alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R2is independently selected from hydrogen, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl, said C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11and SO2R11, said C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-C8heterocycloalkyl, C4-C14alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being further optionally substituted with one or more substituents independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; alternatively R1and R2together with the atoms to which they are attached form a C3-8heterocycloalkyl including 0, 1 or 2 additional ring heteromoieties selected from O, S, S(O), SO2, N and NR11, said C3-8heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-8alkylamino, C1-8alkylsulfonyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; R3is selected from hydrogen, C1-6alkyl, C3-8cycloalkyl, or C4-14 alkylenecycloalkyl; alternatively R3and one of R1and R2together with the atoms to which they are attached form a C3-12 heterocycloalkyl, said C3-12 heterocycloalkyl being further optionally substituted with one or more substituents independently selected from halogen, (O), CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R11, C(O)N(R11)2, OR11, N(R11)2, NO2, SR11, SO2R11, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, N, S(O), SO2and NR11; each R11is independently selected from hydrogen, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl, and C3-7heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12, said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-7cycloalkyl and C3-7heterocycloalkyl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R12, C(O)N(R12)2, OR12, N(R12)2, NO2, SR12and SO2R12, said C3-C7cycloalkyl and C3-7heterocycloalkyl each being further optionally substituted with a substituent independently selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N and NR12; each R12is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C5-10heterocycloalkyl, C6-12aryl and C5-10heteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; R4, R5, R6, R7, R8, R9and R10are each selected from hydrogen, halogen, CN, OR13, N(R13)2, SR13, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, CO2R13, C(O)R13, C(O)N(R13)2, C(O)C(O)N(R13)2, OC(O)R13, OC(O)OR13, OC(O)N(R13)2, OS(O)R13, OS(O)N(R13)2, OSO2R13, OP(O)(OR13)2, OC1-6alkyleneP(O)(OR13)2, S(O)R13, S(O)N(R13)2, SO2R13, N(R13)2, N(R13)C(O)R13, N(R13)C(O)OR13, N(R13)C(O)N(R13)2, NO2, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, C4-16alkyleneheteroaryl; said C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-C6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C1-6alkylamine, C1-6alkoxy, C1-6haloalkoxy, C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2R13, C(O)N(R13)2, OR13, N(R13)2, NO2, SR13and SO2R13, said C3-8cycloalkyl, C3-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C4-16alkyleneheteroaryl each being further optionally substituted with a substituent selected from (O), C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoeities selected from O, S, S(O), SO2, N, and NR13; each R13is independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl,said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, C3-8cycloalkyl, C4-14 alkylenecycloalkyl, C3-10 heterocycloalkyl, C4-16alkyleneheterocycloalkyl, C6-12aryl, C7-18alkylenearyl, C5-10heteroaryl, and C6-16alkyleneheteroaryl each being optionally substituted with one or more substituents independently selected from halogen, CN, C1-8alkoxy, C1-8alkylamino, C1-8alkylsulfonyl, CO2H, CO2CH3, C(O)NH2, C(O)N(CH3)2, C(O)NHCH3, OH, NH2, N(CH3)2, NHCH3, NO2, SH, SCH3, SO2CH3, SOCH3, C1-6alkyl, C1-6haloalkyl, C2-6alkenyl, C2-6haloalkenyl, C2-6alkynyl, C2-6haloalkynyl, C3-6cycloalkyl and C3-6heterocycloalkyl including 1 or 2 ring heteromoieties selected from O, S, S(O), SO2, N, NH and NCH3; wherein at least one of R4, R5, R6and R8is other than hydrogen.

19. A method of treating a mental illness, comprising administering to a subject in need thereof an effective amount of a compound defined in claim 18 or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof.

20. A method of treating a central nervous system (CNS) disease, disorder or condition and / or a neurological disease, disorder or condition, the method comprising administering to a subject in need thereof an effective amount of a compound defined in claim 18 or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof.

21. A method for increasing neuronal plasticity and / or increasing dendritic spine density, the method comprising contacting a neuronal cell with a compound as defined in claim 18 or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof.

22. The method of any one of claims 18 to 21, wherein the compound of formula (I), or a pharmaceutically acceptable salt, solvate, tautomer, N-oxide, stereoisomer, metabolite, polymorph or prodrug thereof, is a compound of any one of claims 1 to 15, optionally administered in the form of the pharmaceutical composition of claim 16 or 17.

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